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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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4150 745 31 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 26218440
5288 745 31 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 26218440
644019 745 31 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 26218440
CHEMBL190461 745 31 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 26218440
DB09061 745 31 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 26218440
10272 1661 19 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 342 5 1 2 5.2 [O-][N+](=O)CC(c1c([nH]c2c1cccc2)c1ccccc1)c1ccccc1 28103441
4402318 1661 19 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 342 5 1 2 5.2 [O-][N+](=O)CC(c1c([nH]c2c1cccc2)c1ccccc1)c1ccccc1 28103441
CHEMBL4450922 1661 19 CNR1 CB1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 342 5 1 2 5.2 [O-][N+](=O)CC(c1c([nH]c2c1cccc2)c1ccccc1)c1ccccc1 28103441
138491556 161783 0 CNR1 CB1 receptor 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 161783 0 CNR1 CB1 receptor 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 167180 0 CNR1 CB1 receptor 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 167180 0 CNR1 CB1 receptor 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
10500128 9163 0 CNR1 CB1 receptor 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 9163 0 CNR1 CB1 receptor 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
138491578 162275 0 CNR1 CB1 receptor 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 162275 0 CNR1 CB1 receptor 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
104850 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 1112 22 CNR1 CB1 receptor 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 1112 22 CNR1 CB1 receptor 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 1112 22 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
104850 3128 84 CNR1 CB1 receptor Rat 9.8 pEC50 = 9.8 Binding
Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorDisplacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1073/pnas.0706980105
4150 3128 84 CNR1 CB1 receptor Rat 9.8 pEC50 = 9.8 Binding
Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorDisplacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1073/pnas.0706980105
743 3128 84 CNR1 CB1 receptor Rat 9.8 pEC50 = 9.8 Binding
Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorDisplacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1073/pnas.0706980105
CHEMBL111 3128 84 CNR1 CB1 receptor Rat 9.8 pEC50 = 9.8 Binding
Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorDisplacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1073/pnas.0706980105
DB06155 3128 84 CNR1 CB1 receptor Rat 9.8 pEC50 = 9.8 Binding
Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorDisplacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1073/pnas.0706980105
10618930 8214 0 CNR1 CB1 receptor 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 8214 0 CNR1 CB1 receptor 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 161999 0 CNR1 CB1 receptor 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 161999 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
104895 1113 19 CNR1 CB1 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment methodAgonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment method
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c01023
730 1113 19 CNR1 CB1 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment methodAgonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment method
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c01023
734 1113 19 CNR1 CB1 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment methodAgonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment method
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL559612 1113 19 CNR1 CB1 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment methodAgonist activity at human CB1 receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay based Tango beta-arrestin recruitment method
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c01023
118720555 115196 0 CNR1 CB1 receptor 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 115196 0 CNR1 CB1 receptor 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 163749 0 CNR1 CB1 receptor 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 163749 0 CNR1 CB1 receptor 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 184250 0 CNR1 CB1 receptor 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 184250 0 CNR1 CB1 receptor 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
CHEMBL510801 207682 12 CNR1 CB1 receptor Rat 9.5 pEC50 = 9.5 Binding
Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorDisplacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor
ChEMBL None None None None 10.1073/pnas.0706980105
CHEMBL4782654 181304 0 CNR1 CB1 receptor 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 103829 0 CNR1 CB1 receptor 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 103829 0 CNR1 CB1 receptor 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 103829 0 CNR1 CB1 receptor 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 103829 0 CNR1 CB1 receptor 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 164682 0 CNR1 CB1 receptor 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 164682 0 CNR1 CB1 receptor 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
145957967 161329 5 CNR1 CB1 receptor 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 161329 5 CNR1 CB1 receptor 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
104895 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 103828 0 CNR1 CB1 receptor 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 103828 0 CNR1 CB1 receptor 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 103828 0 CNR1 CB1 receptor 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 103828 0 CNR1 CB1 receptor 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 116875 1 CNR1 CB1 receptor 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 116875 1 CNR1 CB1 receptor 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 184103 0 CNR1 CB1 receptor 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 184103 0 CNR1 CB1 receptor 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 184164 0 CNR1 CB1 receptor 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 184164 0 CNR1 CB1 receptor 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 186668 0 CNR1 CB1 receptor 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 186668 0 CNR1 CB1 receptor 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 186872 0 CNR1 CB1 receptor 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 186872 0 CNR1 CB1 receptor 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
145984466 164694 0 CNR1 CB1 receptor 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 164694 0 CNR1 CB1 receptor 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 9060 0 CNR1 CB1 receptor 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 9060 0 CNR1 CB1 receptor 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 114472 25 CNR1 CB1 receptor 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 114472 25 CNR1 CB1 receptor 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 163197 0 CNR1 CB1 receptor 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 163197 0 CNR1 CB1 receptor 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 187024 0 CNR1 CB1 receptor 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 187024 0 CNR1 CB1 receptor 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 187831 1 CNR1 CB1 receptor 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 187831 1 CNR1 CB1 receptor 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 188041 0 CNR1 CB1 receptor 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 188041 0 CNR1 CB1 receptor 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 1820 19 CNR1 CB1 receptor 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 1820 19 CNR1 CB1 receptor 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 1820 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 15651 0 CNR1 CB1 receptor 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 15651 0 CNR1 CB1 receptor 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
104895 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 164781 0 CNR1 CB1 receptor 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 164781 0 CNR1 CB1 receptor 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
CHEMBL3416128 117828 0 CNR1 CB1 receptor 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
CHEMBL4779296 181029 0 CNR1 CB1 receptor 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 8181 0 CNR1 CB1 receptor 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 8181 0 CNR1 CB1 receptor 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 156026 0 CNR1 CB1 receptor 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 156026 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
25033940 188105 0 CNR1 CB1 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assayAgonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay
ChEMBL 430 5 1 5 5.3 O=C(CCc1nc(-c2ccc(F)cc2Cl)no1)Nc1cnc2ccc(Cl)cc2c1 10.1021/jm800463f
CHEMBL526345 188105 0 CNR1 CB1 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assayAgonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay
ChEMBL 430 5 1 5 5.3 O=C(CCc1nc(-c2ccc(F)cc2Cl)no1)Nc1cnc2ccc(Cl)cc2c1 10.1021/jm800463f
CHEMBL4760082 180219 0 CNR1 CB1 receptor 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
CHEMBL4787347 181663 0 CNR1 CB1 receptor 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 165066 0 CNR1 CB1 receptor 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 165066 0 CNR1 CB1 receptor 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 190702 0 CNR1 CB1 receptor 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 190702 0 CNR1 CB1 receptor 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 97173 0 CNR1 CB1 receptor 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 97173 0 CNR1 CB1 receptor 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 155264 0 CNR1 CB1 receptor 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 155264 0 CNR1 CB1 receptor 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 155350 0 CNR1 CB1 receptor 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 155350 0 CNR1 CB1 receptor 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 156163 0 CNR1 CB1 receptor 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 156163 0 CNR1 CB1 receptor 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 157555 0 CNR1 CB1 receptor 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 157555 0 CNR1 CB1 receptor 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 158361 0 CNR1 CB1 receptor 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 158361 0 CNR1 CB1 receptor 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 180435 0 CNR1 CB1 receptor 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 180435 0 CNR1 CB1 receptor 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 180436 0 CNR1 CB1 receptor 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 180436 0 CNR1 CB1 receptor 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 181627 0 CNR1 CB1 receptor 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 181627 0 CNR1 CB1 receptor 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 184162 6 CNR1 CB1 receptor 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 184162 6 CNR1 CB1 receptor 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 187024 0 CNR1 CB1 receptor 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 187024 0 CNR1 CB1 receptor 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 187024 0 CNR1 CB1 receptor 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 187024 0 CNR1 CB1 receptor 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 187808 0 CNR1 CB1 receptor 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 187808 0 CNR1 CB1 receptor 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
CHEMBL4781952 181233 0 CNR1 CB1 receptor 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
10024106 95482 0 CNR1 CB1 receptor 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 95482 0 CNR1 CB1 receptor 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
91844670 148627 0 CNR1 CB1 receptor Human 8.9 pEC50 = 8.9 Binding
Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.
ChEMBL 609 6 2 4 6.7 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3945880 148627 0 CNR1 CB1 receptor Human 8.9 pEC50 = 8.9 Binding
Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.
ChEMBL 609 6 2 4 6.7 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL4797581 182467 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 87630 0 CNR1 CB1 receptor 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 87630 0 CNR1 CB1 receptor 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
57780760 85978 1 CNR1 CB1 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 470 8 2 7 3.7 COc1ccc(NC(=O)c2ccc(Cn3ccnn3)c3ccccc23)c(C(=O)NCC2CCC2)n1 10.1021/jm301511h
CHEMBL2316377 85978 1 CNR1 CB1 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 470 8 2 7 3.7 COc1ccc(NC(=O)c2ccc(Cn3ccnn3)c3ccccc23)c(C(=O)NCC2CCC2)n1 10.1021/jm301511h
42625862 187682 0 CNR1 CB1 receptor 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 187682 0 CNR1 CB1 receptor 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 17801 0 CNR1 CB1 receptor 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 17801 0 CNR1 CB1 receptor 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
145959588 161521 0 CNR1 CB1 receptor 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 161521 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
11532254 85989 0 CNR1 CB1 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 440 7 2 6 3.7 O=C(NCC1CCC1)c1ncccc1NC(=O)c1ccc(Cn2ccnn2)c2ccccc12 10.1021/jm301511h
CHEMBL2316387 85989 0 CNR1 CB1 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 440 7 2 6 3.7 O=C(NCC1CCC1)c1ncccc1NC(=O)c1ccc(Cn2ccnn2)c2ccccc12 10.1021/jm301511h
104895 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
104850 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 184165 0 CNR1 CB1 receptor 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 184165 0 CNR1 CB1 receptor 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
CHEMBL4791449 181971 0 CNR1 CB1 receptor 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
CHEMBL3416121 117823 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
155536760 171386 0 CNR1 CB1 receptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assayAgonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assay
ChEMBL 359 7 1 5 3.5 CCCCCn1cc(C(=O)N[C@H](C(=O)OC)C(C)(C)C)c2cccnc21 10.1016/j.ejmech.2019.07.036
CHEMBL4474071 171386 0 CNR1 CB1 receptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assayAgonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assay
ChEMBL 359 7 1 5 3.5 CCCCCn1cc(C(=O)N[C@H](C(=O)OC)C(C)(C)C)c2cccnc21 10.1016/j.ejmech.2019.07.036
155536760 171386 0 CNR1 CB1 receptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assayAgonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assay
ChEMBL 359 7 1 5 3.5 CCCCCn1cc(C(=O)N[C@H](C(=O)OC)C(C)(C)C)c2cccnc21 10.1016/j.ejmech.2019.07.036
CHEMBL4474071 171386 0 CNR1 CB1 receptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assayAgonist activity at human CB1 receptor expressed in AtT-20 cells measured every 2 secs for 2 mins by FLIPR assay
ChEMBL 359 7 1 5 3.5 CCCCCn1cc(C(=O)N[C@H](C(=O)OC)C(C)(C)C)c2cccnc21 10.1016/j.ejmech.2019.07.036
57780750 85977 1 CNR1 CB1 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 498 8 2 7 4.4 COc1ccc(NC(=O)c2ccc(Cn3ccnn3)c3ccccc23)c(C(=O)NCC2CCCCC2)n1 10.1021/jm301511h
CHEMBL2316376 85977 1 CNR1 CB1 receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 498 8 2 7 4.4 COc1ccc(NC(=O)c2ccc(Cn3ccnn3)c3ccccc23)c(C(=O)NCC2CCCCC2)n1 10.1021/jm301511h
155541870 172208 0 CNR1 CB1 receptor 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 172208 0 CNR1 CB1 receptor 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 17803 0 CNR1 CB1 receptor 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 17803 0 CNR1 CB1 receptor 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 73982 0 CNR1 CB1 receptor 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 73982 0 CNR1 CB1 receptor 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 163625 0 CNR1 CB1 receptor 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 163625 0 CNR1 CB1 receptor 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 191397 0 CNR1 CB1 receptor 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 191397 0 CNR1 CB1 receptor 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 62549 0 CNR1 CB1 receptor 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 62549 0 CNR1 CB1 receptor 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 62549 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 158364 0 CNR1 CB1 receptor 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 158364 0 CNR1 CB1 receptor 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 64733 31 CNR1 CB1 receptor 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 64733 31 CNR1 CB1 receptor 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 60485 7 CNR1 CB1 receptor 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 60485 7 CNR1 CB1 receptor 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 62551 0 CNR1 CB1 receptor 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 62551 0 CNR1 CB1 receptor 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 62551 0 CNR1 CB1 receptor 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 109263 0 CNR1 CB1 receptor 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 109263 0 CNR1 CB1 receptor 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
57390958 70063 1 CNR1 CB1 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human CB1 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodAgonist activity at human CB1 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 524 9 0 7 5.9 CCOc1ccc(Cc2nc3cc(N(C)S(=O)(=O)c4cccs4)ccc3n2CC2CCCCC2)nc1 10.1039/C8MD00595H
CHEMBL1950329 70063 1 CNR1 CB1 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human CB1 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodAgonist activity at human CB1 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 524 9 0 7 5.9 CCOc1ccc(Cc2nc3cc(N(C)S(=O)(=O)c4cccs4)ccc3n2CC2CCCCC2)nc1 10.1039/C8MD00595H
11201613 18608 0 CNR1 CB1 receptor 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 18608 0 CNR1 CB1 receptor 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 18608 0 CNR1 CB1 receptor 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 14762 0 CNR1 CB1 receptor 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 14762 0 CNR1 CB1 receptor 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 14762 0 CNR1 CB1 receptor 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
11589652 14762 0 CNR1 CB1 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element 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 10.1039/C0MD00022A
CHEMBL1209647 14762 0 CNR1 CB1 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element 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 10.1039/C0MD00022A
CHEMBL3347358 14762 0 CNR1 CB1 receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element 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 10.1039/C0MD00022A
3929482 92752 6 CNR1 CB1 receptor 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 92752 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 72081 0 CNR1 CB1 receptor 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 72081 0 CNR1 CB1 receptor 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 115854 0 CNR1 CB1 receptor 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 115854 0 CNR1 CB1 receptor 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 180086 0 CNR1 CB1 receptor 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 180086 0 CNR1 CB1 receptor 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 148403 0 CNR1 CB1 receptor 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 148403 0 CNR1 CB1 receptor 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 172208 0 CNR1 CB1 receptor 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 172208 0 CNR1 CB1 receptor 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 170924 0 CNR1 CB1 receptor 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 170924 0 CNR1 CB1 receptor 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 144830 0 CNR1 CB1 receptor 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 144830 0 CNR1 CB1 receptor 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 148403 0 CNR1 CB1 receptor 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 148403 0 CNR1 CB1 receptor 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 151087 0 CNR1 CB1 receptor 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 151087 0 CNR1 CB1 receptor 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 153118 0 CNR1 CB1 receptor 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 153118 0 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 3128 84 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 163967 0 CNR1 CB1 receptor 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 163967 0 CNR1 CB1 receptor 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 142181 0 CNR1 CB1 receptor 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 142181 0 CNR1 CB1 receptor 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 145716 0 CNR1 CB1 receptor 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 145716 0 CNR1 CB1 receptor 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 64723 0 CNR1 CB1 receptor 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 64723 0 CNR1 CB1 receptor 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
52944884 18635 0 CNR1 CB1 receptor 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 18635 0 CNR1 CB1 receptor 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 18642 0 CNR1 CB1 receptor 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 18642 0 CNR1 CB1 receptor 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 18650 0 CNR1 CB1 receptor 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 18650 0 CNR1 CB1 receptor 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 14746 0 CNR1 CB1 receptor 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 14746 0 CNR1 CB1 receptor 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 57724 0 CNR1 CB1 receptor 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 57724 0 CNR1 CB1 receptor 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
59016069 119753 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay
ChEMBL 371 4 0 3 4.1 CCN1CCN(C(=O)c2cn(CC3CCCCC3)c3c(F)cccc23)CC1 10.1039/C0MD00022A
CHEMBL3347302 119753 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay
ChEMBL 371 4 0 3 4.1 CCN1CCN(C(=O)c2cn(CC3CCCCC3)c3c(F)cccc23)CC1 10.1039/C0MD00022A
CHEMBL3545436 119753 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay
ChEMBL 371 4 0 3 4.1 CCN1CCN(C(=O)c2cn(CC3CCCCC3)c3c(F)cccc23)CC1 10.1039/C0MD00022A
24863396 15653 0 CNR1 CB1 receptor 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 15653 0 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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 1113 19 CNR1 CB1 receptor 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
10202883 123044 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Effective concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cellsEffective concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 428 4 1 4 5.2 Cn1c(C(=O)NN2CCCCC2)nc(-c2ccc(Cl)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2004.12.078
CHEMBL362423 123044 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Effective concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cellsEffective concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 428 4 1 4 5.2 Cn1c(C(=O)NN2CCCCC2)nc(-c2ccc(Cl)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2004.12.078
118323987 149444 0 CNR1 CB1 receptor 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 149444 0 CNR1 CB1 receptor 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
CHEMBL4789723 181848 0 CNR1 CB1 receptor 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
118324130 149219 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.
ChEMBL 453 5 1 3 7.4 OC(c1ccc(Cl)cc1)(c1ccc2nccc(/C=C/c3ccccc3)c2c1)c1cccs1 nan
CHEMBL3950371 149219 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7 Binding
Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.Binding Assay: Experimental Procedure CB-1 Membrane Binding: Into Greiner V bottom polypropylene plates, hCB1-CHO-K1 membranes (2 ug/well final concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) were dispensed. Membranes were purchased from Perkin Elmer. Test compounds were then added to each well and then [3H] CP 55, 940 (0.4 nM final well concentration) in assay buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2 and 0.5 mg/ml (0.05%) Ultra fatty acid free BSA) was added. Samples were mixed and incubated for 90 min at 30° C. in the Greiner V Bottom Polypropylene plate. After incubation, assay reagents were transferred to a blocked 384 well polypropylene filter plates. The binding reaction was stopped by filtration and washed seven times with ice cold rinse buffer. Filter plates were then dried overnight at room temperature. The next day, plate bottoms were sealed with plate tape and 15 ul MicroScint 20 was added to each well. Plates were incubated for 2 h and radioactivity was measured by Topcount.
ChEMBL 453 5 1 3 7.4 OC(c1ccc(Cl)cc1)(c1ccc2nccc(/C=C/c3ccccc3)c2c1)c1cccs1 nan
70683294 73012 0 CNR1 CB1 receptor 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 73012 0 CNR1 CB1 receptor 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 83105 0 CNR1 CB1 receptor 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 83105 0 CNR1 CB1 receptor 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 54795 0 CNR1 CB1 receptor 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 54795 0 CNR1 CB1 receptor 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 54795 0 CNR1 CB1 receptor 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
69489327 119778 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay
ChEMBL 431 4 0 3 4.8 CCN1CCN(C(=O)c2cn(CC3CCCCC3)c3cc(Br)ccc23)CC1 10.1039/C0MD00022A
CHEMBL3347292 119778 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay
ChEMBL 431 4 0 3 4.8 CCN1CCN(C(=O)c2cn(CC3CCCCC3)c3cc(Br)ccc23)CC1 10.1039/C0MD00022A
CHEMBL3545577 119778 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay
ChEMBL 431 4 0 3 4.8 CCN1CCN(C(=O)c2cn(CC3CCCCC3)c3cc(Br)ccc23)CC1 10.1039/C0MD00022A
11510814 186269 0 CNR1 CB1 receptor 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 186269 0 CNR1 CB1 receptor 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 116869 0 CNR1 CB1 receptor 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 116869 0 CNR1 CB1 receptor 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 53 32 CNR1 CB1 receptor 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 53 32 CNR1 CB1 receptor 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 53 32 CNR1 CB1 receptor 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 160825 0 CNR1 CB1 receptor 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 160825 0 CNR1 CB1 receptor 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 115388 0 CNR1 CB1 receptor 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 115388 0 CNR1 CB1 receptor 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 191207 0 CNR1 CB1 receptor 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 191207 0 CNR1 CB1 receptor 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 191901 0 CNR1 CB1 receptor 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 191901 0 CNR1 CB1 receptor 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 191902 0 CNR1 CB1 receptor 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 191902 0 CNR1 CB1 receptor 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 190615 0 CNR1 CB1 receptor 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 190615 0 CNR1 CB1 receptor 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 190747 0 CNR1 CB1 receptor 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 190747 0 CNR1 CB1 receptor 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 137578 0 CNR1 CB1 receptor 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 137578 0 CNR1 CB1 receptor 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 150521 0 CNR1 CB1 receptor 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 150521 0 CNR1 CB1 receptor 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
CHEMBL4776615 180817 0 CNR1 CB1 receptor 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
CHEMBL4777738 180901 0 CNR1 CB1 receptor 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
CHEMBL4781040 181168 0 CNR1 CB1 receptor 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
CHEMBL4781576 181208 0 CNR1 CB1 receptor 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
CHEMBL4781800 181225 0 CNR1 CB1 receptor 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
CHEMBL4782074 181248 0 CNR1 CB1 receptor 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
CHEMBL4783974 181411 0 CNR1 CB1 receptor 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
CHEMBL4784418 181460 0 CNR1 CB1 receptor 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
CHEMBL4785185 181510 0 CNR1 CB1 receptor 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
CHEMBL4785295 181515 0 CNR1 CB1 receptor 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
CHEMBL4786352 181586 0 CNR1 CB1 receptor 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
CHEMBL4787759 181690 0 CNR1 CB1 receptor 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
CHEMBL4788470 181748 0 CNR1 CB1 receptor 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
CHEMBL4788749 181769 0 CNR1 CB1 receptor 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
CHEMBL4790368 181904 0 CNR1 CB1 receptor 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
CHEMBL4790704 181926 0 CNR1 CB1 receptor 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
CHEMBL4791040 181946 0 CNR1 CB1 receptor 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
CHEMBL4791212 181954 0 CNR1 CB1 receptor 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
CHEMBL4791388 181964 0 CNR1 CB1 receptor 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 182017 0 CNR1 CB1 receptor 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 182017 0 CNR1 CB1 receptor 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
CHEMBL4793164 182096 0 CNR1 CB1 receptor 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
CHEMBL4793976 182162 0 CNR1 CB1 receptor 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
CHEMBL4795529 182296 0 CNR1 CB1 receptor 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
CHEMBL4795667 182310 0 CNR1 CB1 receptor 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
CHEMBL4796542 182388 0 CNR1 CB1 receptor 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
CHEMBL4797039 182423 0 CNR1 CB1 receptor 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
CHEMBL4797941 182502 0 CNR1 CB1 receptor 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
CHEMBL4798902 182570 0 CNR1 CB1 receptor 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 73992 0 CNR1 CB1 receptor 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 73992 0 CNR1 CB1 receptor 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
60155823 76405 0 CNR1 CB1 receptor 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 76405 0 CNR1 CB1 receptor 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
67953300 114950 0 CNR1 CB1 receptor 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 114950 0 CNR1 CB1 receptor 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 149624 0 CNR1 CB1 receptor 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 149624 0 CNR1 CB1 receptor 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 146640 0 CNR1 CB1 receptor 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 146640 0 CNR1 CB1 receptor 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 159153 0 CNR1 CB1 receptor 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 159153 0 CNR1 CB1 receptor 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 70065 0 CNR1 CB1 receptor 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 70065 0 CNR1 CB1 receptor 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 70074 0 CNR1 CB1 receptor 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 70074 0 CNR1 CB1 receptor 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 143416 0 CNR1 CB1 receptor 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 143416 0 CNR1 CB1 receptor 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
CHEMBL4799912 182654 0 CNR1 CB1 receptor 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 360 45 CNR1 CB1 receptor 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 360 45 CNR1 CB1 receptor 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 360 45 CNR1 CB1 receptor 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 172070 0 CNR1 CB1 receptor 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 172070 0 CNR1 CB1 receptor 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
25053215 184767 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP bindingAntagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding
ChEMBL 524 4 1 5 6.4 Cc1c(C(=O)NN2CC3CCCC3C2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(C#CC2CC2)s1 10.1021/jm800066v
CHEMBL493917 184767 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP bindingAntagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding
ChEMBL 524 4 1 5 6.4 Cc1c(C(=O)NN2CC3CCCC3C2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(C#CC2CC2)s1 10.1021/jm800066v
118710162 112847 0 CNR1 CB1 receptor Human 5.0 pEC50 = 5.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 1036 18 4 8 11.7 Cc1c(C(=O)NCCCCNC(=O)[C@H]2CCCC[C@@H]2C(=O)NCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322465 112847 0 CNR1 CB1 receptor Human 5.0 pEC50 = 5.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 1036 18 4 8 11.7 Cc1c(C(=O)NCCCCNC(=O)[C@H]2CCCC[C@@H]2C(=O)NCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
118720565 115209 0 CNR1 CB1 receptor 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 115209 0 CNR1 CB1 receptor 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 84380 1 CNR1 CB1 receptor 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 84380 1 CNR1 CB1 receptor 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
118710162 112847 0 CNR1 CB1 receptor Human 5.0 pEC50 = 5.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 1036 18 4 8 11.7 Cc1c(C(=O)NCCCCNC(=O)[C@H]2CCCC[C@@H]2C(=O)NCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322465 112847 0 CNR1 CB1 receptor Human 5.0 pEC50 = 5.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 1036 18 4 8 11.7 Cc1c(C(=O)NCCCCNC(=O)[C@H]2CCCC[C@@H]2C(=O)NCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
53324282 56547 0 CNR1 CB1 receptor 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 56547 0 CNR1 CB1 receptor 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 2785 69 CNR1 CB1 receptor 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 2785 69 CNR1 CB1 receptor 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 2785 69 CNR1 CB1 receptor 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
155527981 170445 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 360 5 1 2 5.4 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4460580 170445 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 360 5 1 2 5.4 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.9b01142
71093593 142049 0 CNR1 CB1 receptor 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 142049 0 CNR1 CB1 receptor 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 144858 0 CNR1 CB1 receptor 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 144858 0 CNR1 CB1 receptor 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 144858 0 CNR1 CB1 receptor 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 144858 0 CNR1 CB1 receptor 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
118710170 112854 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 560 9 2 4 7.0 Cc1c(C(=O)NCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322473 112854 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 560 9 2 4 7.0 Cc1c(C(=O)NCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
118710171 112855 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 616 13 2 4 8.6 Cc1c(C(=O)NCCCCCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322474 112855 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 616 13 2 4 8.6 Cc1c(C(=O)NCCCCCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
22475020 95317 14 CNR1 CB1 receptor 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 95317 14 CNR1 CB1 receptor 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 158717 0 CNR1 CB1 receptor 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 158717 0 CNR1 CB1 receptor 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 70083 0 CNR1 CB1 receptor 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 70083 0 CNR1 CB1 receptor 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
16737690 85983 0 CNR1 CB1 receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 646 11 2 10 3.9 O=C(NCC1CCOCC1)c1nc(OS(=O)(=O)CCC(F)(F)F)ccc1NC(=O)c1ccc(Cn2ccnn2)c2ccccc12 10.1021/jm301511h
CHEMBL2316381 85983 0 CNR1 CB1 receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 646 11 2 10 3.9 O=C(NCC1CCOCC1)c1nc(OS(=O)(=O)CCC(F)(F)F)ccc1NC(=O)c1ccc(Cn2ccnn2)c2ccccc12 10.1021/jm301511h
16078 1271 16 CNR1 CB1 receptor 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 1271 16 CNR1 CB1 receptor 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 1271 16 CNR1 CB1 receptor 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 1271 16 CNR1 CB1 receptor 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 1271 16 CNR1 CB1 receptor 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 149324 0 CNR1 CB1 receptor 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 149324 0 CNR1 CB1 receptor 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 150686 0 CNR1 CB1 receptor 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 150686 0 CNR1 CB1 receptor 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 184165 0 CNR1 CB1 receptor 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 184165 0 CNR1 CB1 receptor 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 142181 0 CNR1 CB1 receptor 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 142181 0 CNR1 CB1 receptor 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 142951 0 CNR1 CB1 receptor 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 142951 0 CNR1 CB1 receptor 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 145716 0 CNR1 CB1 receptor 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 145716 0 CNR1 CB1 receptor 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 104127 0 CNR1 CB1 receptor 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 104127 0 CNR1 CB1 receptor 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 114968 0 CNR1 CB1 receptor 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 114968 0 CNR1 CB1 receptor 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
5311501 3833 6 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm301511h
733 3833 6 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm301511h
CHEMBL188 3833 6 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm301511h
DB13950 3833 6 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assayAgonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay
ChEMBL 426 4 0 5 4.6 O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2 10.1021/jm301511h
118710170 112854 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 560 9 2 4 7.0 Cc1c(C(=O)NCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322473 112854 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 560 9 2 4 7.0 Cc1c(C(=O)NCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
155553407 173282 0 CNR1 CB1 receptor 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 173282 0 CNR1 CB1 receptor 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 149293 0 CNR1 CB1 receptor 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 149293 0 CNR1 CB1 receptor 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 114969 0 CNR1 CB1 receptor 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 114969 0 CNR1 CB1 receptor 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
25034071 185465 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assayAgonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay
ChEMBL 417 6 0 5 5.7 Fc1ccc(-c2noc(CCCOc3cnc4ccc(Cl)cc4c3)n2)c(Cl)c1 10.1021/jm800463f
CHEMBL498469 185465 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assayAgonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay
ChEMBL 417 6 0 5 5.7 Fc1ccc(-c2noc(CCCOc3cnc4ccc(Cl)cc4c3)n2)c(Cl)c1 10.1021/jm800463f
44586998 185524 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assayAgonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay
ChEMBL 466 7 1 6 6.0 Fc1ccc(-c2noc(CCCNc3ccc4ncc(OC(F)(F)F)cc4c3)n2)c(Cl)c1 10.1021/jm800463f
CHEMBL499066 185524 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assayAgonist activity at human CB1 receptor expressed in Sf9 cells by GTP-europium binding assay
ChEMBL 466 7 1 6 6.0 Fc1ccc(-c2noc(CCCNc3ccc4ncc(OC(F)(F)F)cc4c3)n2)c(Cl)c1 10.1021/jm800463f
123627357 162119 0 CNR1 CB1 receptor 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 162119 0 CNR1 CB1 receptor 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 176065 0 CNR1 CB1 receptor 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 176065 0 CNR1 CB1 receptor 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 188754 1 CNR1 CB1 receptor 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 188754 1 CNR1 CB1 receptor 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 188781 1 CNR1 CB1 receptor 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 188781 1 CNR1 CB1 receptor 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 147120 0 CNR1 CB1 receptor 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 147120 0 CNR1 CB1 receptor 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
118710171 112855 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 616 13 2 4 8.6 Cc1c(C(=O)NCCCCCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322474 112855 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 616 13 2 4 8.6 Cc1c(C(=O)NCCCCCCCCNC(=O)C2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
155513497 168931 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 378 5 1 2 5.5 O=[N+]([O-])CC(c1ccc(F)cc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4438948 168931 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 378 5 1 2 5.5 O=[N+]([O-])CC(c1ccc(F)cc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
155533629 171039 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccc(F)cc1)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4469368 171039 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccc(F)cc1)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12 10.1021/acs.jmedchem.9b01142
155553407 173282 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin 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 173282 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 360 5 1 2 5.4 O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
155544651 172497 0 CNR1 CB1 receptor 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 172497 0 CNR1 CB1 receptor 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 174797 0 CNR1 CB1 receptor 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 174797 0 CNR1 CB1 receptor 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 147120 0 CNR1 CB1 receptor 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 147120 0 CNR1 CB1 receptor 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 149461 0 CNR1 CB1 receptor 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 149461 0 CNR1 CB1 receptor 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 149017 0 CNR1 CB1 receptor 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 149017 0 CNR1 CB1 receptor 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
155536120 171296 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assayPositive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assay
ChEMBL 356 4 1 1 6.5 N#CCC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(Cl)ccc12 10.1021/acs.jmedchem.9b00252
CHEMBL4473034 171296 0 CNR1 CB1 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assayPositive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assay
ChEMBL 356 4 1 1 6.5 N#CCC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(Cl)ccc12 10.1021/acs.jmedchem.9b00252
11690547 139894 0 CNR1 CB1 receptor 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 139894 0 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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 3833 6 CNR1 CB1 receptor 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
118710064 112832 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 506 11 2 4 6.8 Cc1c(C(=O)NCCCCCCCCN)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322349 112832 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 506 11 2 4 6.8 Cc1c(C(=O)NCCCCCCCCN)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
118710064 112832 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 506 11 2 4 6.8 Cc1c(C(=O)NCCCCCCCCN)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
CHEMBL3322349 112832 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assayInverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
ChEMBL 506 11 2 4 6.8 Cc1c(C(=O)NCCCCCCCCN)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.07.038
53394452 142825 9 CNR1 CB1 receptor Mouse 7.0 pEC50 = 7.0 Binding
[35S]GTPγS Binding Assay: [35S]GTPγS binding was performed as previously described [Brents et al., PLoS One, 6:e21917]. Briefly, 25 μg of mouse brain homogenates were incubated for 30 minutes at 30° C. with 0.1 nM [35S]GTPγS, 10 μM GDP, and either cannabinoid+/−antagonist, 10 μM unlabeled GTPγS (non-specific binding) or vehicle (total binding), in triplicate, in a volume of 1 mL of buffer containing 20 mM HEPES, 10 mM MgCl2, 100 mM NaCl, 20 units/L adenosine deaminase, 0.05% BSA and the appropriate DMSO (0.1%) and/or ethanol (<0.2%) vehicle. Assay buffer containing 100 mM KCl, instead of 100 mM NaCl, was used to increase basal G-protein activity in experiments examining inverse agonism. Reactions were terminated by quick vacuum filtration through Whatman GF/B glass fiber filters, followed by five washes with ice-cold buffer (20 mM HEPES, 0.05% BSA). Filters were immediately placed into 7 mL scintillation vials to which 4 mL of ScintiVerse™ BD Cocktail scintillation fluid was added. Bound radioactivity was determined after overnight incubation at room temperature and shaking by liquid scintillation spectrophotometry with an efficiency of 93% (Tri Carb 2100 TR Liquid Scintillation Analyzer, Packard Instrument Company, Meriden, Conn.).[35S]GTPγS Binding Assay: [35S]GTPγS binding was performed as previously described [Brents et al., PLoS One, 6:e21917]. Briefly, 25 μg of mouse brain homogenates were incubated for 30 minutes at 30° C. with 0.1 nM [35S]GTPγS, 10 μM GDP, and either cannabinoid+/−antagonist, 10 μM unlabeled GTPγS (non-specific binding) or vehicle (total binding), in triplicate, in a volume of 1 mL of buffer containing 20 mM HEPES, 10 mM MgCl2, 100 mM NaCl, 20 units/L adenosine deaminase, 0.05% BSA and the appropriate DMSO (0.1%) and/or ethanol (<0.2%) vehicle. Assay buffer containing 100 mM KCl, instead of 100 mM NaCl, was used to increase basal G-protein activity in experiments examining inverse agonism. Reactions were terminated by quick vacuum filtration through Whatman GF/B glass fiber filters, followed by five washes with ice-cold buffer (20 mM HEPES, 0.05% BSA). Filters were immediately placed into 7 mL scintillation vials to which 4 mL of ScintiVerse™ BD Cocktail scintillation fluid was added. Bound radioactivity was determined after overnight incubation at room temperature and shaking by liquid scintillation spectrophotometry with an efficiency of 93% (Tri Carb 2100 TR Liquid Scintillation Analyzer, Packard Instrument Company, Meriden, Conn.).
ChEMBL 343 5 1 3 5.5 CCCCn1cc(C(=O)c2cccc3ccccc23)c2c(O)cccc21 nan
CHEMBL3899761 142825 9 CNR1 CB1 receptor Mouse 7.0 pEC50 = 7.0 Binding
[35S]GTPγS Binding Assay: [35S]GTPγS binding was performed as previously described [Brents et al., PLoS One, 6:e21917]. Briefly, 25 μg of mouse brain homogenates were incubated for 30 minutes at 30° C. with 0.1 nM [35S]GTPγS, 10 μM GDP, and either cannabinoid+/−antagonist, 10 μM unlabeled GTPγS (non-specific binding) or vehicle (total binding), in triplicate, in a volume of 1 mL of buffer containing 20 mM HEPES, 10 mM MgCl2, 100 mM NaCl, 20 units/L adenosine deaminase, 0.05% BSA and the appropriate DMSO (0.1%) and/or ethanol (<0.2%) vehicle. Assay buffer containing 100 mM KCl, instead of 100 mM NaCl, was used to increase basal G-protein activity in experiments examining inverse agonism. Reactions were terminated by quick vacuum filtration through Whatman GF/B glass fiber filters, followed by five washes with ice-cold buffer (20 mM HEPES, 0.05% BSA). Filters were immediately placed into 7 mL scintillation vials to which 4 mL of ScintiVerse™ BD Cocktail scintillation fluid was added. Bound radioactivity was determined after overnight incubation at room temperature and shaking by liquid scintillation spectrophotometry with an efficiency of 93% (Tri Carb 2100 TR Liquid Scintillation Analyzer, Packard Instrument Company, Meriden, Conn.).[35S]GTPγS Binding Assay: [35S]GTPγS binding was performed as previously described [Brents et al., PLoS One, 6:e21917]. Briefly, 25 μg of mouse brain homogenates were incubated for 30 minutes at 30° C. with 0.1 nM [35S]GTPγS, 10 μM GDP, and either cannabinoid+/−antagonist, 10 μM unlabeled GTPγS (non-specific binding) or vehicle (total binding), in triplicate, in a volume of 1 mL of buffer containing 20 mM HEPES, 10 mM MgCl2, 100 mM NaCl, 20 units/L adenosine deaminase, 0.05% BSA and the appropriate DMSO (0.1%) and/or ethanol (<0.2%) vehicle. Assay buffer containing 100 mM KCl, instead of 100 mM NaCl, was used to increase basal G-protein activity in experiments examining inverse agonism. Reactions were terminated by quick vacuum filtration through Whatman GF/B glass fiber filters, followed by five washes with ice-cold buffer (20 mM HEPES, 0.05% BSA). Filters were immediately placed into 7 mL scintillation vials to which 4 mL of ScintiVerse™ BD Cocktail scintillation fluid was added. Bound radioactivity was determined after overnight incubation at room temperature and shaking by liquid scintillation spectrophotometry with an efficiency of 93% (Tri Carb 2100 TR Liquid Scintillation Analyzer, Packard Instrument Company, Meriden, Conn.).
ChEMBL 343 5 1 3 5.5 CCCCn1cc(C(=O)c2cccc3ccccc23)c2c(O)cccc21 nan
117923246 136868 0 CNR1 CB1 receptor 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 136868 0 CNR1 CB1 receptor 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 142050 0 CNR1 CB1 receptor 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 142050 0 CNR1 CB1 receptor 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 82999 0 CNR1 CB1 receptor 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 82999 0 CNR1 CB1 receptor 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 165887 0 CNR1 CB1 receptor 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 165887 0 CNR1 CB1 receptor 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
155514785 169039 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assayPositive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assay
ChEMBL 429 5 1 3 6.8 COC(=O)c1ccc2c(C(CC(F)(F)F)c3cccs3)c(-c3ccccc3)[nH]c2c1 10.1021/acs.jmedchem.9b00252
CHEMBL4440510 169039 0 CNR1 CB1 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assayPositive allosteric modulation of human CB1 receptor expressed in CHOK1 cells assessed as increase in CP55940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55940 addition and measured after 90 to 180 mins by PathHunter assay
ChEMBL 429 5 1 3 6.8 COC(=O)c1ccc2c(C(CC(F)(F)F)c3cccs3)c(-c3ccccc3)[nH]c2c1 10.1021/acs.jmedchem.9b00252
118324113 144298 0 CNR1 CB1 receptor 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 144298 0 CNR1 CB1 receptor 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 147911 0 CNR1 CB1 receptor 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 147911 0 CNR1 CB1 receptor 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 76402 0 CNR1 CB1 receptor 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 76402 0 CNR1 CB1 receptor 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
155537440 171481 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 378 5 1 2 5.5 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4475358 171481 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced beta-arrestin2 recruitment after 90 mins in presence of CP55940 at EC20 concentration by pathhunter beta-arrestin assay
ChEMBL 378 5 1 2 5.5 O=[N+]([O-])CC(c1ccccc1F)c1c(-c2ccccc2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
71525480 143583 0 CNR1 CB1 receptor 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 143583 0 CNR1 CB1 receptor 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
11854358 70066 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 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 419 5 0 3 5.2 C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(CC1CCCC1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950332 70066 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 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 419 5 0 3 5.2 C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(CC1CCCC1)CC2 10.1016/j.bmcl.2011.12.124
71087454 159388 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 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.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 377 4 2 3 3.4 CNC(=O)[C@@H](NC(=O)c1cccc(-c2ccc(F)c(Cl)c2)n1)C(C)(C)C nan
CHEMBL4109654 159388 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 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.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 377 4 2 3 3.4 CNC(=O)[C@@H](NC(=O)c1cccc(-c2ccc(F)c(Cl)c2)n1)C(C)(C)C nan
145990629 166072 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 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 441 6 1 4 5.6 O=c1cc(OCc2ccccc2)c2cc(C(c3ccc(Cl)cc3)n3ccnc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL4286211 166072 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 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 441 6 1 4 5.6 O=c1cc(OCc2ccccc2)c2cc(C(c3ccc(Cl)cc3)n3ccnc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
155540863 171653 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 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 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccc(F)cc1)c1c(-c2cccc(F)c2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
CHEMBL4483342 171653 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 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 396 5 1 2 5.7 O=[N+]([O-])CC(c1ccc(F)cc1)c1c(-c2cccc(F)c2)[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.9b01142
57398026 70078 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayPartial agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 451 4 0 5 4.5 CCCC(=O)n1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950345 70078 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayPartial agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 451 4 0 5 4.5 CCCC(=O)n1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2 10.1016/j.bmcl.2011.12.124
46873203 115056 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant CB1 receptor expressing CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at human recombinant CB1 receptor expressing CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 361 3 1 4 4.6 CC(C)(C)c1cc(NC(=O)[C@@H]2CCCCN2c2ccc(Cl)cc2)no1 10.1016/j.bmcl.2014.12.031
CHEMBL3354527 115056 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant CB1 receptor expressing CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at human recombinant CB1 receptor expressing CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 361 3 1 4 4.6 CC(C)(C)c1cc(NC(=O)[C@@H]2CCCCN2c2ccc(Cl)cc2)no1 10.1016/j.bmcl.2014.12.031
118329964 143455 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 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 536 5 2 6 6.2 CC(C)(C)OC(=O)N1CC[C@H](Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4nccs4)cc23)C1 nan
CHEMBL3904867 143455 0 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 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 536 5 2 6 6.2 CC(C)(C)OC(=O)N1CC[C@H](Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4nccs4)cc23)C1 nan
24125805 169851 2 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Binding
Antagonist activity at N-terminal Flag epitope tagged CB1 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assayAntagonist activity at N-terminal Flag epitope tagged CB1 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assay
ChEMBL 286 2 1 3 3.6 Cc1nc(C)c(C(=O)NC2CCCc3ccccc32)s1 10.1016/j.ejmech.2019.07.002
CHEMBL4451793 169851 2 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Binding
Antagonist activity at N-terminal Flag epitope tagged CB1 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assayAntagonist activity at N-terminal Flag epitope tagged CB1 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assay
ChEMBL 286 2 1 3 3.6 Cc1nc(C)c(C(=O)NC2CCCc3ccccc32)s1 10.1016/j.ejmech.2019.07.002
5066764 181138 15 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulatory activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production preincubated for 30 mins followed by CP55940 addition and measured after 60 mins by Hit-hunter assayPositive allosteric modulatory activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production preincubated for 30 mins followed by CP55940 addition and measured after 60 mins by Hit-hunter assay
ChEMBL 372 6 1 3 5.3 COc1ccc(C(C[N+](=O)[O-])c2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/j.bmc.2020.115727
CHEMBL4780669 181138 15 CNR1 CB1 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulatory activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production preincubated for 30 mins followed by CP55940 addition and measured after 60 mins by Hit-hunter assayPositive allosteric modulatory activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production preincubated for 30 mins followed by CP55940 addition and measured after 60 mins by Hit-hunter assay
ChEMBL 372 6 1 3 5.3 COc1ccc(C(C[N+](=O)[O-])c2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/j.bmc.2020.115727
123233001 136996 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 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 415 5 2 5 5.7 O=C(Nc1ccc(N=C=S)cc1)Nc1cccc(-c2cccc(N3CCCC3)n2)c1 10.1021/acs.jmedchem.5b01303
CHEMBL3759542 136996 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 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 415 5 2 5 5.7 O=C(Nc1ccc(N=C=S)cc1)Nc1cccc(-c2cccc(N3CCCC3)n2)c1 10.1021/acs.jmedchem.5b01303
46871948 92333 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human recombinant CB1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at human recombinant CB1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 378 6 0 3 5.6 CCCCCn1c2ccc(C(=O)N3CCCCC3)cc2c2ccc(OC)cc21 10.1016/j.ejmech.2013.09.038
CHEMBL2441475 92333 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human recombinant CB1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at human recombinant CB1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 378 6 0 3 5.6 CCCCCn1c2ccc(C(=O)N3CCCCC3)cc2c2ccc(OC)cc21 10.1016/j.ejmech.2013.09.038
CHEMBL4790621 181919 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulatory activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production preincubated for 30 mins followed by CP55940 addition and measured after 60 mins by Hit-hunter assayPositive allosteric modulatory activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production preincubated for 30 mins followed by CP55940 addition and measured after 60 mins by Hit-hunter assay
ChEMBL 348 5 1 3 5.3 O=[N+]([O-])CC(c1ccsc1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1016/j.bmc.2020.115727
CHEMBL4757488 180013 0 CNR1 CB1 receptor Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayPartial agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay
ChEMBL 450 5 1 3 5.6 Cc1c(-c2ccc(F)cc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
44437862 91316 0 CNR1 CB1 receptor Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contractionAgonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction
ChEMBL 511 5 1 3 5.2 CC12CCC(C1)C(C)(C)C2NC(=O)C1=NS(=O)(=O)N(Cc2ccccc2)C(c2ccc(Cl)cc2)=C1 10.1016/j.bmc.2007.07.056
CHEMBL241567 91316 0 CNR1 CB1 receptor Mouse 4.9 pEC50 = 4.9 Functional
Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contractionAgonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction
ChEMBL 511 5 1 3 5.2 CC12CCC(C1)C(C)(C)C2NC(=O)C1=NS(=O)(=O)N(Cc2ccccc2)C(c2ccc(Cl)cc2)=C1 10.1016/j.bmc.2007.07.056
49780793 17800 0 CNR1 CB1 receptor Rat 5.9 pEC50 = 5.9 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 967 22 3 7 13.6 Cc1c(C(=O)NCCCCCCCNCCCCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1021/jm1006676
CHEMBL1269766 17800 0 CNR1 CB1 receptor Rat 5.9 pEC50 = 5.9 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 967 22 3 7 13.6 Cc1c(C(=O)NCCCCCCCNCCCCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1021/jm1006676
11544639 96975 32 CNR1 CB1 receptor Rat 7.9 pEC50 = 7.9 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 339 4 0 3 4.9 CC1(C)C(C(=O)c2cn(CC3CCOCC3)c3ccccc23)C1(C)C 10.1021/jm901214q