Ligand source activities (1 row/activity)





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2536 199365 40 None 6918 3 Human 9.5 pAC50 = 9.5 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 398 7 3 6 1.4 CN(C)C(=O)COC(=O)Cc1ccc(OC(=O)c2ccc(NC(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL590799 199365 40 None 6918 3 Human 9.5 pAC50 = 9.5 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 398 7 3 6 1.4 CN(C)C(=O)COC(=O)Cc1ccc(OC(=O)c2ccc(NC(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
2519 779 86 None 58 8 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
407 779 86 None 58 8 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
463 779 86 None 58 8 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL113 779 86 None 58 8 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
DB00201 779 86 None 58 8 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1038/s41467-023-40064-9
2997 193151 35 None 13 4 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 270 1 1 2 3.1 O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1 10.1038/s41467-023-40064-9
CHEMBL523 193151 35 None 13 4 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 270 1 1 2 3.1 O=C1CN=C(c2ccccc2)c2cc(Cl)ccc2N1 10.1038/s41467-023-40064-9
5411 204033 89 None 5370 11 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL698 204033 89 None 5370 11 Human 9.2 pAC50 = 9.2 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
1610 2347 95 None 9 11 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 422 8 2 6 4.3 CCCCc1nc(c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CO)Cl 10.1038/s41467-023-40064-9
3941 2347 95 None 9 11 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 422 8 2 6 4.3 CCCCc1nc(c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CO)Cl 10.1038/s41467-023-40064-9
3961 2347 95 None 9 11 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 422 8 2 6 4.3 CCCCc1nc(c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CO)Cl 10.1038/s41467-023-40064-9
590 2347 95 None 9 11 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 422 8 2 6 4.3 CCCCc1nc(c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CO)Cl 10.1038/s41467-023-40064-9
CHEMBL191 2347 95 None 9 11 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 422 8 2 6 4.3 CCCCc1nc(c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CO)Cl 10.1038/s41467-023-40064-9
DB00678 2347 95 None 9 11 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 422 8 2 6 4.3 CCCCc1nc(c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CO)Cl 10.1038/s41467-023-40064-9
2540 4401 111 None -87 28 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4401 111 None -87 28 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
2132 46224 91 None 5248 4 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 376 3 3 3 3.2 Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1 10.1038/s41467-023-40064-9
CHEMBL1514634 46224 91 None 5248 4 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 376 3 3 3 3.2 Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1 10.1038/s41467-023-40064-9
CHEMBL153479 46224 91 None 5248 4 Human 8.9 pAC50 = 8.9 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 376 3 3 3 3.2 Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1 10.1038/s41467-023-40064-9
4150 788 39 None -16 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 788 39 None -16 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 788 39 None -16 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 788 39 None -16 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 788 39 None -16 15 Human 6.0 pAC50 = 6.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
1016 3747 78 None -1445 40 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 3747 78 None -1445 40 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 3747 78 None -1445 40 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 3747 78 None -1445 40 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 3747 78 None -1445 40 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 3747 78 None -1445 40 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5282219 35869 63 None -1 9 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 450 12 1 5 5.7 CC(C)=CCOc1ccc(/C=C/C(=O)c2ccc(OCC=C(C)C)cc2OCC(=O)O)cc1 10.1038/s41467-023-40064-9
CHEMBL1441961 35869 63 None -1 9 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 450 12 1 5 5.7 CC(C)=CCOc1ccc(/C=C/C(=O)c2ccc(OCC=C(C)C)cc2OCC(=O)O)cc1 10.1038/s41467-023-40064-9
65016 10209 86 None -1 3 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 505 11 3 7 2.4 CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)c1ccc(N)cc1 10.1038/s41467-023-40064-9
CHEMBL116 10209 86 None -1 3 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 505 11 3 7 2.4 CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)c1ccc(N)cc1 10.1038/s41467-023-40064-9
4499 59775 99 None -5 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
CHEMBL1726 59775 99 None -5 8 Human 4.9 pAC50 = 4.9 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
51755 57406 54 None -1 10 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1651990 57406 54 None -1 10 Human 5.9 pAC50 = 5.9 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
2880 98008 49 None -14 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL27289 98008 49 None -14 9 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
1530 2182 50 None -1148 25 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2182 50 None -1148 25 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2182 50 None -1148 25 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2182 50 None -1148 25 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2182 50 None -1148 25 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
2540 4401 111 None -87 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4401 111 None -87 28 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
60065 84369 6 None -10 11 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2218858 84369 6 None -10 11 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
1862 2710 13 None -1 3 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 372 6 1 3 6.3 CCCCCCC(c1cc(O)c2c(c1)OC(C1C2CC(=O)CC1)(C)C)(C)C 10.1038/s41467-023-40064-9
39860 2710 13 None -1 3 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 372 6 1 3 6.3 CCCCCCC(c1cc(O)c2c(c1)OC(C1C2CC(=O)CC1)(C)C)(C)C 10.1038/s41467-023-40064-9
9071 2710 13 None -1 3 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 372 6 1 3 6.3 CCCCCCC(c1cc(O)c2c(c1)OC(C1C2CC(=O)CC1)(C)C)(C)C 10.1038/s41467-023-40064-9
CHEMBL2218896 2710 13 None -1 3 Human 6.8 pAC50 = 6.8 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 372 6 1 3 6.3 CCCCCCC(c1cc(O)c2c(c1)OC(C1C2CC(=O)CC1)(C)C)(C)C 10.1038/s41467-023-40064-9
3149 12614 15 None -46 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12614 15 None -46 26 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
107751 78143 103 None -1 2 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 9 1 5 3.0 CC(=O)SCC(Cc1ccccc1)C(=O)NCC(=O)OCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL2103772 78143 103 None -1 2 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 385 9 1 5 3.0 CC(=O)SCC(Cc1ccccc1)C(=O)NCC(=O)OCc1ccccc1 10.1038/s41467-023-40064-9
2335 11848 22 None -131 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11848 22 None -131 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11848 22 None -131 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11848 22 None -131 34 Human 4.8 pAC50 = 4.8 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3478 5426 103 None 213 4 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 445 7 3 6 2.1 Cc1cnc(C(=O)NCCc2ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc2)cn1 10.1038/s41467-023-40064-9
CHEMBL1073 5426 103 None 213 4 Human 7.7 pAC50 = 7.7 Functional
Compound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assayCompound was evaluated for inhibition of human CNR1 in an in vitro assay with cellular components measured by membrane filtration, radioligand displacement assay
ChEMBL 445 7 3 6 2.1 Cc1cnc(C(=O)NCCc2ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc2)cn1 10.1038/s41467-023-40064-9
4046 2483 33 None -42 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 33 None -42 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 33 None -42 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 33 None -42 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
72093 35061 9 None -17 28 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35061 9 None -17 28 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35061 9 None -17 28 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
2407 3372 76 None -6025 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3372 76 None -6025 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3372 76 None -6025 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3372 76 None -6025 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3372 76 None -6025 17 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
2435 3590 83 None -4897 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 83 None -4897 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 83 None -4897 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 83 None -4897 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 83 None -4897 21 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
236702 45730 63 None -1 2 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 434 3 2 6 2.5 CC(=O)OCC(=O)[C@@]1(O)[C@H](C)C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1530428 45730 63 None -1 2 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 434 3 2 6 2.5 CC(=O)OCC(=O)[C@@]1(O)[C@H](C)C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
4507 180678 101 None -1 2 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 360 5 1 7 2.6 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL475534 180678 101 None -1 2 Human 4.7 pAC50 = 4.7 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 360 5 1 7 2.6 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
11980903 14492 19 None -630 25 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14492 19 None -630 25 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14492 19 None -630 25 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14492 19 None -630 25 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
3949 100614 50 None -24 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100614 50 None -24 16 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
118422671 2757 65 None -7943 23 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2757 65 None -7943 23 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2757 65 None -7943 23 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2757 65 None -7943 23 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2757 65 None -7943 23 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2757 65 None -7943 23 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
4008 7226 92 None -7 6 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 610 10 1 9 5.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL1085699 7226 92 None -7 6 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 610 10 1 9 5.0 COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
636403 188268 22 None -10 7 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL499915 188268 22 None -10 7 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
11658860 2344 51 None -229 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
2941 2344 51 None -229 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
4374 2344 51 None -229 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
CHEMBL360328 2344 51 None -229 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
DB04871 2344 51 None -229 11 Human 5.6 pAC50 = 5.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 195 0 1 1 2.6 Clc1ccc2c(c1)[C@@H](C)CNCC2 10.1038/s41467-023-40064-9
5077 3578 79 None -1071 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
7552 3578 79 None -1071 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
9913767 3578 79 None -1071 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL238804 3578 79 None -1071 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
DB11362 3578 79 None -1071 13 Human 4.6 pAC50 = 4.6 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
5280453 205971 74 None -8 8 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 416 6 3 3 5.7 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL846 205971 74 None -8 8 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 416 6 3 3 5.7 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
4046 2483 33 None -42 17 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 33 None -42 17 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 33 None -42 17 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 33 None -42 17 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
2855 4132 104 None -15135 12 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
3322 4132 104 None -15135 12 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
5717 4132 104 None -15135 12 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL603 4132 104 None -15135 12 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
DB00549 4132 104 None -15135 12 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
444254 49613 24 None - 1 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 645 9 14 19 -8.6 C[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O[C@H]3[C@H](O)[C@@H](O)[C@H](O)O[C@@H]3CO)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1N[C@H]1C=C(CO)[C@@H](O)[C@H](O)[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL1566 49613 24 None - 1 Human 4.5 pAC50 = 4.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 645 9 14 19 -8.6 C[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O[C@H]3[C@H](O)[C@@H](O)[C@H](O)O[C@@H]3CO)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1N[C@H]1C=C(CO)[C@@H](O)[C@H](O)[C@H]1O 10.1038/s41467-023-40064-9
3947 206395 53 None -7 16 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 206395 53 None -7 16 Human 5.5 pAC50 = 5.5 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
636374 14451 41 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 520 6 1 7 3.9 CCC(=O)OCC(=O)[C@@]1(OC(=O)CC)[C@H](C)C[C@H]2[C@H]3[C@H]([C@@H](O)C[C@@]21C)[C@@]1(C)C=CC(=O)C=C1C[C@H]3Cl 10.1038/s41467-023-40064-9
CHEMBL1200989 14451 41 None - 1 Human 6.2 pAC50 = 6.2 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 520 6 1 7 3.9 CCC(=O)OCC(=O)[C@@]1(OC(=O)CC)[C@H](C)C[C@H]2[C@H]3[C@H]([C@@H](O)C[C@@]21C)[C@@]1(C)C=CC(=O)C=C1C[C@H]3Cl 10.1038/s41467-023-40064-9
104850 3330 96 None 1 27 Human 8.1 pAC50 = 8.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3330 96 None 1 27 Human 8.1 pAC50 = 8.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3330 96 None 1 27 Human 8.1 pAC50 = 8.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3330 96 None 1 27 Human 8.1 pAC50 = 8.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3330 96 None 1 27 Human 8.1 pAC50 = 8.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4034 55822 55 None -9 18 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55822 55 None -9 18 Human 5.1 pAC50 = 5.1 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
135564886 14493 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14493 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14493 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14493 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14493 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14493 5 None -3 25 Human 5.0 pAC50 = 5.0 Functional
Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135 2532 43 None -4466 33 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 43 None -4466 33 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 43 None -4466 33 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 43 None -4466 33 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 43 None -4466 33 Human 5.0 pAC50 = 5.0 Functional
Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
164611580 184537 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 395 3 1 6 2.1 O=C(NC12CCC(CC1)CC2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4847866 184537 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 395 3 1 6 2.1 O=C(NC12CCC(CC1)CC2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
164625379 186236 0 None 831 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 391 3 1 6 2.7 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4873473 186236 0 None 831 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 391 3 1 6 2.7 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
138491556 162608 0 None 15 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 383 15 1 2 6.0 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC1CC1 10.1021/acs.jmedchem.8b00243
CHEMBL4169198 162608 0 None 15 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 383 15 1 2 6.0 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC1CC1 10.1021/acs.jmedchem.8b00243
156248679 185491 0 None 14454 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 393 3 1 6 2.7 O=C(NC1(C(F)(F)F)CCC1)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4862304 185491 0 None 14454 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 393 3 1 6 2.7 O=C(NC1(C(F)(F)F)CCC1)c1nn(-c2cnccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
156248933 186389 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 366 4 0 8 3.2 CCC(C)(C)c1noc(-c2nn(-c3cnccn3)c3c2CC2CCC3O2)n1 10.1021/acsmedchemlett.1c00331
CHEMBL4875720 186389 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 366 4 0 8 3.2 CCC(C)(C)c1noc(-c2nn(-c3cnccn3)c3c2CC2CCC3O2)n1 10.1021/acsmedchemlett.1c00331
164609298 184461 0 None 35481 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 353 3 1 6 1.0 O=C(NC12CC(C1)C2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4846759 184461 0 None 35481 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 353 3 1 6 1.0 O=C(NC12CC(C1)C2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
164621737 185684 0 None 2187 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 384 2 0 8 2.5 CC(C)(C)c1nnc(-c2nn(-c3c[n+]([O-])ccn3)c3c2CC2CCC3O2)s1 10.1021/acsmedchemlett.1c00331
CHEMBL4865162 185684 0 None 2187 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 384 2 0 8 2.5 CC(C)(C)c1nnc(-c2nn(-c3c[n+]([O-])ccn3)c3c2CC2CCC3O2)s1 10.1021/acsmedchemlett.1c00331
138491578 163100 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 16 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC(C)CO 10.1021/acs.jmedchem.8b00243
CHEMBL4177060 163100 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 16 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC(C)CO 10.1021/acs.jmedchem.8b00243
164619069 186182 0 None 8 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 425 3 1 4 4.2 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4872695 186182 0 None 8 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 425 3 1 4 4.2 O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL5091754 215324 0 None 4 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC(C)(CCCCCCC#N)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC[C@@H](CO)C[C@@H]21 10.1021/acs.jmedchem.0c02053
164620714 186084 0 None 4677 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@H]1CC[C@@H]2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4871491 186084 0 None 4677 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@H]1CC[C@@H]2O1 10.1021/acsmedchemlett.1c00331
CHEMBL5081770 214766 0 None 7 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC(C)(CCCCCCN=[N+]=[N-])c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC[C@@H](CO)C[C@@H]21 10.1021/acs.jmedchem.0c02053
104850 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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
138491579 162824 0 None 38 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 17 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCCO 10.1021/acs.jmedchem.8b00243
CHEMBL4172580 162824 0 None 38 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 401 17 2 3 5.2 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCCO 10.1021/acs.jmedchem.8b00243
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/jm070317a
118720555 115939 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method
ChEMBL 389 5 1 3 4.4 CC(C)(NC(=O)c1nn(Cc2ccc(F)cc2)c2c1C[C@H]1C[C@@H]21)c1ccccc1 10.1016/j.bmcl.2014.11.040
CHEMBL3354941 115939 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method
ChEMBL 389 5 1 3 4.4 CC(C)(NC(=O)c1nn(Cc2ccc(F)cc2)c2c1C[C@H]1C[C@@H]21)c1ccccc1 10.1016/j.bmcl.2014.11.040
24945480 186928 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 426 4 0 3 3.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccccc1 10.1021/jm900063x
CHEMBL490024 186928 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 426 4 0 3 3.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccccc1 10.1021/jm900063x
CHEMBL5071417 214258 0 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC1(C)Oc2cc(C3(CCCCCCC#N)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/acs.jmedchem.0c02053
162664878 182178 0 None 46 2 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assayAntagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assay
ChEMBL 432 5 1 3 5.5 Cc1c(-c2ccccc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
CHEMBL4782654 182178 0 None 46 2 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assayAntagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assay
ChEMBL 432 5 1 3 5.5 Cc1c(-c2ccccc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
CHEMBL5074603 214320 0 None -1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC1(C)Oc2cc(C3(CCCCCCCN=C=S)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/acs.jmedchem.0c02053
145957967 162153 11 None 52 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 387 16 2 3 4.8 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCO 10.1021/acs.jmedchem.8b00243
CHEMBL4161934 162153 11 None 52 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay
ChEMBL 387 16 2 3 4.8 CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCO 10.1021/acs.jmedchem.8b00243
86274158 192690 15 None 26 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assay
ChEMBL 367 8 1 3 4.8 CC(C)(NC(=O)c1nn(CCCCCF)c2ccccc12)c1ccccc1 10.1021/acs.jmedchem.2c00969
CHEMBL5219235 192690 15 None 26 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assay
ChEMBL 367 8 1 3 4.8 CC(C)(NC(=O)c1nn(CCCCCF)c2ccccc12)c1ccccc1 10.1021/acs.jmedchem.2c00969
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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
46239964 117623 1 None -12 2 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 396 3 1 5 4.4 CC(C)(C)c1cc(NC(=O)[C@]2(C)CCCN2c2ccc(C(F)(F)F)cn2)no1 10.1016/j.bmcl.2014.12.033
CHEMBL3400946 117623 1 None -12 2 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 396 3 1 5 4.4 CC(C)(C)c1cc(NC(=O)[C@]2(C)CCCN2c2ccc(C(F)(F)F)cn2)no1 10.1016/j.bmcl.2014.12.033
24945636 186780 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 5 0 3 4.5 O=C(CCc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
CHEMBL489031 186780 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 5 0 3 4.5 O=C(CCc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
24944972 186842 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 404 3 0 3 3.4 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
CHEMBL489429 186842 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 404 3 0 3 3.4 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
24945479 189516 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 480 4 0 3 4.1 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
CHEMBL514068 189516 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 480 4 0 3 4.1 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1 10.1021/jm900063x
24945635 189721 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 437 4 0 4 2.9 N#Cc1ccc(CC(=O)N2CCN(S(=O)(=O)c3cc(Cl)cc(Cl)c3)CC2)cc1 10.1021/jm900063x
CHEMBL515641 189721 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 437 4 0 4 2.9 N#Cc1ccc(CC(=O)N2CCN(S(=O)(=O)c3cc(Cl)cc(Cl)c3)CC2)cc1 10.1021/jm900063x
CHEMBL5092703 215382 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL None None None CC1(C)Oc2cc(C3(CCCCCCN=C=S)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/acs.jmedchem.0c02053
164620733 186087 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@@H]1CC[C@H]2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4871528 186087 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 371 4 2 7 1.6 CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@@H]1CC[C@H]2O1 10.1021/acsmedchemlett.1c00331
107778 115214 33 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(CO)C[C@H]21 10.1021/jm0503906
CHEMBL334533 115214 33 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(CO)C[C@H]21 10.1021/jm0503906
3868445 193166 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 386 3 0 3 3.3 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm900063x
CHEMBL523100 193166 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 386 3 0 3 3.3 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm900063x
24944801 193375 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 414 3 0 3 4.0 CC1(C)CN(S(=O)(=O)c2cccc3ccccc23)CCN1C(=O)C1CCCCC1 10.1021/jm900063x
CHEMBL525204 193375 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 414 3 0 3 4.0 CC1(C)CN(S(=O)(=O)c2cccc3ccccc23)CCN1C(=O)C1CCCCC1 10.1021/jm900063x
731 1947 24 None -2 3 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 1947 24 None -2 3 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 1947 24 None -2 3 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 16010 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 395 6 1 2 5.9 CCCCCC1=NN(C(=O)N[C@H]2C[C@H]3CC[C@]2(C)C3(C)C)CC1c1ccccc1 10.1016/j.bmcl.2010.07.056
CHEMBL1223588 16010 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 395 6 1 2 5.9 CCCCCC1=NN(C(=O)N[C@H]2C[C@H]3CC[C@]2(C)C3(C)C)CC1c1ccccc1 10.1016/j.bmcl.2010.07.056
155907792 189902 5 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
CHEMBL5169682 189902 5 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
155907792 189902 5 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
CHEMBL5169682 189902 5 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 6 2 4 2.5 CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21 10.1039/d1md00242b
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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
44177373 8448 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 459 4 1 2 6.1 Cc1ccc(C(c2ccc(Cl)cc2Cl)N2CCN(C(=O)NC3CCCCC3)CC2)cc1 10.1016/j.ejmech.2009.12.018
CHEMBL1093735 8448 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
ChEMBL 459 4 1 2 6.1 Cc1ccc(C(c2ccc(Cl)cc2Cl)N2CCN(C(=O)NC3CCCCC3)CC2)cc1 10.1016/j.ejmech.2009.12.018
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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
45101490 197111 0 None 301 2 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 514 8 2 4 6.3 C[C@H](NC(=O)C(C)(C)Nc1cc(C(F)(F)F)ccn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
CHEMBL567679 197111 0 None 301 2 Human 9.1 pEC50 = 9.1 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 514 8 2 4 6.3 C[C@H](NC(=O)C(C)(C)Nc1cc(C(F)(F)F)ccn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
24768473 97862 0 None 2 3 Mouse 9.0 pEC50 = 9 Functional
Activity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formationActivity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formation
ChEMBL 416 4 1 4 5.3 Cc1c(C(=O)NC2CCCCC2)nn(-c2ccc(Cl)c(Cl)c2)c1-n1cccc1 10.1021/jm070566z
CHEMBL272203 97862 0 None 2 3 Mouse 9.0 pEC50 = 9 Functional
Activity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formationActivity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formation
ChEMBL 416 4 1 4 5.3 Cc1c(C(=O)NC2CCCCC2)nn(-c2ccc(Cl)c(Cl)c2)c1-n1cccc1 10.1021/jm070566z
42625791 181309 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 548 4 0 3 4.8 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL476253 181309 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 548 4 0 3 4.8 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
42625463 181310 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 558 4 0 3 4.6 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Br)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL476254 181310 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 558 4 0 3 4.6 O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Br)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
24945235 182502 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 538 5 0 5 3.6 COC(=O)c1cc(C(F)(F)F)cc(S(=O)(=O)N2CCN(C(=O)Cc3ccc(C(F)(F)F)cc3)CC2)c1 10.1021/jm900063x
CHEMBL478696 182502 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 538 5 0 5 3.6 COC(=O)c1cc(C(F)(F)F)cc(S(=O)(=O)N2CCN(C(=O)Cc3ccc(C(F)(F)F)cc3)CC2)c1 10.1021/jm900063x
2729564 186840 6 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 472 3 0 3 4.1 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
CHEMBL489425 186840 6 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 472 3 0 3 4.1 O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm900063x
24744027 189873 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 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 189873 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 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 189873 0 None - 1 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 189873 0 None - 1 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 193142 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 364 3 0 3 2.7 Cc1cc(C)cc(S(=O)(=O)N2CCN(C(=O)C3CCCCC3)CC2)c1 10.1021/jm900063x
CHEMBL522930 193142 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 364 3 0 3 2.7 Cc1cc(C)cc(S(=O)(=O)N2CCN(C(=O)C3CCCCC3)CC2)c1 10.1021/jm900063x
162665228 182106 0 None 2 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayAgonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay
ChEMBL 390 4 1 3 4.5 Cc1c(Cl)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
CHEMBL4781952 182106 0 None 2 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayAgonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay
ChEMBL 390 4 1 3 4.5 Cc1c(Cl)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.ejmech.2020.112858
104895 1184 25 None -9 8 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c02053
730 1184 25 None -9 8 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c02053
734 1184 25 None -9 8 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c02053
CHEMBL559612 1184 25 None -9 8 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.0c02053
10024106 96169 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 403 3 0 3 5.1 O=C(c1cc2c(cc1F)OC(c1ccccc1)(c1ccccc1)O2)N1CCCCC1 10.1021/jm701487t
CHEMBL260625 96169 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 403 3 0 3 5.1 O=C(c1cc2c(cc1F)OC(c1ccccc1)(c1ccccc1)O2)N1CCCCC1 10.1021/jm701487t
156248392 184380 0 None 89 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 361 2 1 4 3.5 CC(C)(C)NC(=O)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
CHEMBL4845707 184380 0 None 89 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 361 2 1 4 3.5 CC(C)(C)NC(=O)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1 10.1021/acsmedchemlett.1c00331
162676369 183344 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)
ChEMBL 396 7 2 3 4.7 CN(C)c1ccc(CCNC(=O)c2[nH]c3ccc(Cl)cc3c2CN=[N+]=[N-])cc1 10.1016/j.ejmech.2016.05.044
CHEMBL4797581 183344 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)
ChEMBL 396 7 2 3 4.7 CN(C)c1ccc(CCNC(=O)c2[nH]c3ccc(Cl)cc3c2CN=[N+]=[N-])cc1 10.1016/j.ejmech.2016.05.044
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 88298 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 396 2 2 3 5.5 CC1(C)Oc2cc(C34CC5CC(CC(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/jm4000775
CHEMBL2348462 88298 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 mins
ChEMBL 396 2 2 3 5.5 CC1(C)Oc2cc(C34CC5CC(CC(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21 10.1021/jm4000775
42625862 192756 0 None - 1 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 192756 0 None - 1 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
164887460 192141 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 395 6 1 4 5.9 CC1(C)Oc2cc(C3(CCCCCC#N)CCC3)cc(O)c2[C@@H]2CC(=O)CC[C@H]21 10.1016/j.ejmech.2021.114027
CHEMBL5203712 192141 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 395 6 1 4 5.9 CC1(C)Oc2cc(C3(CCCCCC#N)CCC3)cc(O)c2[C@@H]2CC(=O)CC[C@H]21 10.1016/j.ejmech.2021.114027
145959588 162346 0 None -1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 434 4 1 3 4.6 Cc1c(Br)cn(Cc2ccc(F)cc2)c(=O)c1C(=O)NC1CCCCCC1 10.1016/j.ejmech.2018.05.019
CHEMBL4164954 162346 0 None -1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay
ChEMBL 434 4 1 3 4.6 Cc1c(Br)cn(Cc2ccc(F)cc2)c(=O)c1C(=O)NC1CCCCCC1 10.1016/j.ejmech.2018.05.019
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1021/acs.jmedchem.9b01142
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.bmc.2014.07.006
104895 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.114027
730 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.114027
734 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.114027
CHEMBL559612 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.114027
104850 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 186843 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 4 0 3 4.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1 10.1021/jm900063x
CHEMBL489437 186843 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level
ChEMBL 494 4 0 3 4.6 CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1 10.1021/jm900063x
104895 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.113354
730 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.113354
734 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.113354
CHEMBL559612 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.ejmech.2021.113354
162672230 182847 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 8 1 5 3.3 CCCCCn1nc(C(=O)N[C@@H](C(=O)OC)C(C)C)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4791449 182847 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 8 1 5 3.3 CCCCCn1nc(C(=O)N[C@@H](C(=O)OC)C(C)C)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
ChEMBL 376 10 3 3 5.7 CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C 10.1016/j.bmc.2020.115513
155541870 173051 0 None - 1 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 173051 0 None - 1 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
57606063 74567 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 437 6 1 4 3.5 CCN(CC(=O)NC1CC1)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
CHEMBL2029727 74567 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 437 6 1 4 3.5 CCN(CC(=O)NC1CC1)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
45487312 197807 0 None 26 2 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 496 8 2 4 6.5 C[C@H](NC(=O)C(C)(C)Nc1cc2ccccc2cn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
CHEMBL572097 197807 0 None 26 2 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
ChEMBL 496 8 2 4 6.5 C[C@H](NC(=O)C(C)(C)Nc1cc2ccccc2cn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1 10.1016/j.bmcl.2009.07.046
54580071 63102 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 461 9 1 6 5.2 CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO 10.1016/j.bmcl.2011.02.023
CHEMBL1762814 63102 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 461 9 1 6 5.2 CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO 10.1016/j.bmcl.2011.02.023
CHEMBL1789190 63102 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 461 9 1 6 5.2 CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO 10.1016/j.bmcl.2011.02.023
104895 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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
54752945 65289 38 None -1 2 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 65289 38 None -1 2 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 61032 10 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 8 1 6 5.0 CC(C)N(CCO)Cc1csc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)n1 10.1016/j.bmcl.2011.02.023
CHEMBL1762808 61032 10 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 8 1 6 5.0 CC(C)N(CCO)Cc1csc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)n1 10.1016/j.bmcl.2011.02.023
54582096 63104 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 8 1 6 5.7 CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl 10.1016/j.bmcl.2011.02.023
CHEMBL1762816 63104 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 8 1 6 5.7 CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl 10.1016/j.bmcl.2011.02.023
CHEMBL1789209 63104 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 8 1 6 5.7 CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl 10.1016/j.bmcl.2011.02.023
25195469 109989 0 None -10 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay
ChEMBL 420 4 1 4 3.8 O=C(NC1CCCC1)c1ccc2c(c1)N(S(=O)(=O)c1ccc(F)cc1)CCS2 10.1021/jm4005626
CHEMBL3234688 109989 0 None -10 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay
ChEMBL 420 4 1 4 3.8 O=C(NC1CCCC1)c1ccc2c(c1)N(S(=O)(=O)c1ccc(F)cc1)CCS2 10.1021/jm4005626
11201613 18983 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 407 2 0 4 4.5 O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1 10.1016/j.bmcl.2010.10.061
CHEMBL1287847 18983 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 407 2 0 4 4.5 O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1 10.1016/j.bmcl.2010.10.061
CHEMBL1287876 18983 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 407 2 0 4 4.5 O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1 10.1016/j.bmcl.2010.10.061
11589652 15115 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 411 5 0 4 4.8 CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C 10.1016/j.bmcl.2010.06.067
CHEMBL1209647 15115 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 411 5 0 4 4.8 CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C 10.1016/j.bmcl.2010.06.067
CHEMBL3347358 15115 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 411 5 0 4 4.8 CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C 10.1016/j.bmcl.2010.06.067
3929482 93424 18 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 0 5 3.9 Cc1ccc(C(=O)Oc2cccc3cccnc23)cc1S(=O)(=O)N1CCCCC1 10.1016/j.bmcl.2006.09.049
CHEMBL245876 93424 18 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 0 5 3.9 Cc1ccc(C(=O)Oc2cccc3cccnc23)cc1S(=O)(=O)N1CCCCC1 10.1016/j.bmcl.2006.09.049
118916083 180959 0 None 165 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay
ChEMBL 654 11 3 6 7.2 O=C(COc1nc(NCc2cccc(C(F)(F)F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2n1)NCCO 10.1021/acsmedchemlett.0c00495
CHEMBL4758427 180959 0 None 165 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay
ChEMBL 654 11 3 6 7.2 O=C(COc1nc(NCc2cccc(C(F)(F)F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2n1)NCCO 10.1021/acsmedchemlett.0c00495
118329970 149204 0 None 83 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3943971 149204 0 None 83 2 Human 8.0 pEC50 = 8 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
118324097 145632 0 None 5 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 687 6 2 4 7.5 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)cc(Br)c2[nH]1 nan
CHEMBL3915692 145632 0 None 5 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 687 6 2 4 7.5 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)cc(Br)c2[nH]1 nan
118329970 149204 0 None 83 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 nan
CHEMBL3943971 149204 0 None 83 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 619 6 2 6 5.8 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1 nan
118329975 151889 0 None 416 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 587 6 2 3 7.4 O=C(CC(F)(F)F)N1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
CHEMBL3965825 151889 0 None 416 2 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 587 6 2 3 7.4 O=C(CC(F)(F)F)N1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
118329979 153920 0 None - 1 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 522 5 2 2 8.6 O=c1cc(Nc2ccc(F)c(Cl)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
CHEMBL3983340 153920 0 None - 1 Human 8.0 pEC50 = 8 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 522 5 2 2 8.6 O=c1cc(Nc2ccc(F)c(Cl)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 nan
104850 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 3330 96 None 1 27 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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 1184 25 None -9 8 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
118323946 142983 0 None 371 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 555 6 2 5 6.9 O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3894411 142983 0 None 371 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 555 6 2 5 6.9 O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
118324060 146517 0 None 602 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 610 6 2 5 6.1 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
CHEMBL3922599 146517 0 None 602 2 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 610 6 2 5 6.1 O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1 10.1021/acs.jmedchem.8b01467
56642428 65279 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 342 6 0 3 5.6 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccncc21 10.1016/j.ejmech.2011.08.021
CHEMBL1828632 65279 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release
ChEMBL 342 6 0 3 5.6 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccncc21 10.1016/j.ejmech.2011.08.021
155535617 172066 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
CHEMBL4472094 172066 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
52944884 19011 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3CCN4CCCC[C@@H]4C3)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288054 19011 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3CCN4CCCC[C@@H]4C3)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
52943703 19018 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288114 19018 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
52944916 19026 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 423 4 0 4 4.9 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4CC3(C)C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288176 19026 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 423 4 0 4 4.9 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4CC3(C)C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
49862566 15099 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 367 2 0 4 3.5 CN1CCN(C(=O)c2cn3c4c(cccc24)OC[C@H]3C2CCCCC2)CC1 10.1016/j.bmcl.2010.06.067
CHEMBL1209576 15099 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 367 2 0 4 3.5 CN1CCN(C(=O)c2cn3c4c(cccc24)OC[C@H]3C2CCCCC2)CC1 10.1016/j.bmcl.2010.06.067
53326154 58252 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 400 5 0 6 4.4 Clc1cccc2c(-c3noc(CN4CCCC4)n3)cn(CC3CCOCC3)c12 10.1016/j.bmcl.2011.01.082
CHEMBL1682271 58252 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay
ChEMBL 400 5 0 6 4.4 Clc1cccc2c(-c3noc(CN4CCCC4)n3)cn(CC3CCOCC3)c12 10.1016/j.bmcl.2011.01.082
24863396 16012 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 399 6 1 2 5.6 CCCCC1=NN(C(=O)NC(C)(C)c2ccc(F)cc2)CC1c1cccc(F)c1 10.1016/j.bmcl.2010.07.056
CHEMBL1223590 16012 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay
ChEMBL 399 6 1 2 5.6 CCCCC1=NN(C(=O)NC(C)(C)c2ccc(F)cc2)CC1c1cccc(F)c1 10.1016/j.bmcl.2010.07.056
CHEMBL5092514 215373 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins in presence of forskolin by HitHunter chemiluminescence based assayPositive allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins in presence of forskolin by HitHunter chemiluminescence based assay
ChEMBL None None None O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccoc2)[nH]c2ccccc12 10.1016/j.bmc.2021.116421
118323987 150246 0 None 2 2 Human 7.0 pEC50 = 7 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 623 7 1 5 7.5 COc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
CHEMBL3952365 150246 0 None 2 2 Human 7.0 pEC50 = 7 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 623 7 1 5 7.5 COc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
162668450 182724 0 None -10 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 295 6 2 4 2.5 CCCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4789723 182724 0 None -10 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 295 6 2 4 2.5 CCCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
70683294 73593 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CB1 receptorAgonist activity at CB1 receptor
ChEMBL 549 8 2 9 2.5 O=C(NCCO)C1CCN(Cc2nc(-c3cn(CC4CCS(=O)(=O)CC4)c4c(Cl)cccc34)no2)CC1 10.1016/j.bmcl.2012.02.048
CHEMBL2017689 73593 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at CB1 receptorAgonist activity at CB1 receptor
ChEMBL 549 8 2 9 2.5 O=C(NCCO)C1CCN(Cc2nc(-c3cn(CC4CCS(=O)(=O)CC4)c4c(Cl)cccc34)no2)CC1 10.1016/j.bmcl.2012.02.048
71454145 83755 0 None -70 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay
ChEMBL 456 3 1 4 4.9 O=C(Nc1sc2c(c1C(=O)N1CCCCC1)CCOC2)c1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2012.10.087
CHEMBL2205617 83755 0 None -70 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay
ChEMBL 456 3 1 4 4.9 O=C(Nc1sc2c(c1C(=O)N1CCCCC1)CCOC2)c1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2012.10.087
52941290 55301 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1288145 55301 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
CHEMBL1618454 55301 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay
ChEMBL 409 4 0 4 4.5 COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12 10.1016/j.bmcl.2010.10.061
11510814 189110 0 None 20 2 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity
ChEMBL 454 4 1 5 5.6 Cc1c(C(=O)NN2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1 10.1016/j.bmcl.2009.03.046
CHEMBL510262 189110 0 None 20 2 Human 6.0 pEC50 = 6 Functional
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity
ChEMBL 454 4 1 5 5.6 Cc1c(C(=O)NN2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1 10.1016/j.bmcl.2009.03.046
118728139 117617 0 None -707 2 Human 6.0 pEC50 = 6 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 450 2 1 4 4.1 O=C(Nc1cc(C(F)(F)F)on1)N1CCCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2014.12.033
CHEMBL3400938 117617 0 None -707 2 Human 6.0 pEC50 = 6 Functional
Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 450 2 1 4 4.1 O=C(Nc1cc(C(F)(F)F)on1)N1CCCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2014.12.033
141463776 161651 0 None -63 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assayAgonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay
ChEMBL 370 7 2 4 4.5 CCCCNc1cc(C(C)C)c(C(=O)NC23CC4CC(CC(C4)C2)C3)nn1 10.1016/j.ejmech.2017.05.060
CHEMBL4130290 161651 0 None -63 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assayAgonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay
ChEMBL 370 7 2 4 4.5 CCCCNc1cc(C(C)C)c(C(=O)NC23CC4CC(CC(C4)C2)C3)nn1 10.1016/j.ejmech.2017.05.060
118722160 116131 0 None -478 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 464 5 2 7 1.7 CC(C)(C)Cc1nc2cc(S(=O)(=O)C3CN(C(N)=O)C3)ccc2n1CC1(O)CCOCC1 10.1016/j.bmcl.2014.11.062
CHEMBL3357387 116131 0 None -478 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 464 5 2 7 1.7 CC(C)(C)Cc1nc2cc(S(=O)(=O)C3CN(C(N)=O)C3)ccc2n1CC1(O)CCOCC1 10.1016/j.bmcl.2014.11.062
45486215 197617 0 None -125 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 433 3 0 4 4.9 O=C(c1cc(-c2cccc(Cl)c2Cl)cnc1N1CCCCCC1)N1CCOCC1 10.1016/j.bmcl.2009.10.041
CHEMBL570683 197617 0 None -125 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 433 3 0 4 4.9 O=C(c1cc(-c2cccc(Cl)c2Cl)cnc1N1CCCCCC1)N1CCOCC1 10.1016/j.bmcl.2009.10.041
45486166 198311 0 None -251 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 320 2 0 2 5.4 Clc1cccc(-c2ccc(N3CCCCCC3)nc2)c1Cl 10.1016/j.bmcl.2009.10.041
CHEMBL576079 198311 0 None -251 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 320 2 0 2 5.4 Clc1cccc(-c2ccc(N3CCCCCC3)nc2)c1Cl 10.1016/j.bmcl.2009.10.041
45375898 198312 0 None -100 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 345 2 0 3 5.3 N#Cc1cc(N2CCCCCC2)ncc1-c1cccc(Cl)c1Cl 10.1016/j.bmcl.2009.10.041
CHEMBL576087 198312 0 None -100 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells
ChEMBL 345 2 0 3 5.3 N#Cc1cc(N2CCCCCC2)ncc1-c1cccc(Cl)c1Cl 10.1016/j.bmcl.2009.10.041
44475348 197023 0 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 384 3 1 5 3.8 Cc1cn(C)c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
CHEMBL567087 197023 0 None -15 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 384 3 1 5 3.8 Cc1cn(C)c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
11689242 197156 0 None -912 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 370 3 2 4 3.7 Cc1c[nH]c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
CHEMBL567911 197156 0 None -912 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry
ChEMBL 370 3 2 4 3.7 Cc1c[nH]c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12 10.1021/jm9009857
71105652 151323 0 None -776 2 Human 5.0 pEC50 = 5 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 419 8 1 7 2.9 Cc1nc(C(NC(=O)c2ccc(N3CC(F)(F)C3)c(OCC3CC3)n2)C2CC2)no1 nan
CHEMBL3960990 151323 0 None -776 2 Human 5.0 pEC50 = 5 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 419 8 1 7 2.9 Cc1nc(C(NC(=O)c2ccc(N3CC(F)(F)C3)c(OCC3CC3)n2)C2CC2)no1 nan
162643760 181692 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 315 4 2 4 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4776615 181692 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 315 4 2 4 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccc2)n1 10.1021/acs.jmedchem.0c01023
162644317 181776 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(=O)NCc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4777738 181776 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(=O)NCc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
162663645 182042 0 None -144 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 333 4 2 4 2.8 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4781040 182042 0 None -144 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 333 4 2 4 2.8 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2)n1 10.1021/acs.jmedchem.0c01023
162664518 182082 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 317 4 2 6 1.5 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncccn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4781576 182082 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 317 4 2 6 1.5 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncccn2)n1 10.1021/acs.jmedchem.0c01023
162664931 182099 0 None -57 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 4 2 4 2.9 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2F)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4781800 182099 0 None -57 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 351 4 2 4 2.9 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2F)n1 10.1021/acs.jmedchem.0c01023
162665007 182121 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(C)(C)C)cc1C(=O)Nc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4782074 182121 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(C)(C)C)cc1C(=O)Nc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
162666213 182285 0 None -512 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 329 4 2 4 3.0 Cc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4783974 182285 0 None -512 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 329 4 2 4 3.0 Cc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
162666580 182334 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 345 5 2 5 2.7 COc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4784418 182334 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 345 5 2 5 2.7 COc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01023
162666392 182384 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(C)(C)C)cc1C(=O)NCc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
CHEMBL4785185 182384 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 361 7 1 3 5.0 CCCCCn1nc(C(C)(C)C)cc1C(=O)NCc1ccc(Cl)cc1 10.1021/acs.jmedchem.0c01023
162665956 182389 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 371 6 1 3 5.1 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c01023
CHEMBL4785295 182389 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 371 6 1 3 5.1 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c01023
162667222 182461 0 None -489 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 349 4 2 4 3.3 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4786352 182461 0 None -489 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 349 4 2 4 3.3 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cc2)n1 10.1021/acs.jmedchem.0c01023
162669636 182566 0 None -549 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 299 6 2 4 2.0 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(CCCF)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4787759 182566 0 None -549 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 299 6 2 4 2.0 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(CCCF)n1 10.1021/acs.jmedchem.0c01023
162623028 182624 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 383 4 2 4 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(C(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4788470 182624 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 383 4 2 4 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(C(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
162668533 182645 0 None -33 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 365 8 2 4 3.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1-c1ccc(F)cc1F 10.1021/acs.jmedchem.0c01023
CHEMBL4788749 182645 0 None -33 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 365 8 2 4 3.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1-c1ccc(F)cc1F 10.1021/acs.jmedchem.0c01023
162668965 182780 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 335 8 2 4 3.6 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CCCCC1 10.1021/acs.jmedchem.0c01023
CHEMBL4790368 182780 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 335 8 2 4 3.6 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CCCCC1 10.1021/acs.jmedchem.0c01023
162671037 182802 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2cccnc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4790704 182802 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2cccnc2)n1 10.1021/acs.jmedchem.0c01023
162671764 182822 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 387 6 2 4 4.2 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(O)(C3)C1)C2 10.1021/acs.jmedchem.0c01023
CHEMBL4791040 182822 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 387 6 2 4 4.2 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(O)(C3)C1)C2 10.1021/acs.jmedchem.0c01023
162671765 182830 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 8 2 4 2.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CC1 10.1021/acs.jmedchem.0c01023
CHEMBL4791212 182830 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 8 2 4 2.5 CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CC1 10.1021/acs.jmedchem.0c01023
162671780 182840 0 None -13 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 350 4 2 5 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4791388 182840 0 None -13 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 350 4 2 5 2.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cn2)n1 10.1021/acs.jmedchem.0c01023
141747275 182893 0 None -331 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 5 1 3 3.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4792134 182893 0 None -331 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 293 5 1 3 3.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)C 10.1021/acs.jmedchem.0c01023
162671856 182972 0 None -316 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 309 7 2 4 2.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)CO 10.1021/acs.jmedchem.0c01023
CHEMBL4793164 182972 0 None -316 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 309 7 2 4 2.9 CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)CO 10.1021/acs.jmedchem.0c01023
162672350 183038 0 None -741 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 334 4 2 5 2.2 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4793976 183038 0 None -741 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 334 4 2 5 2.2 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cn2)n1 10.1021/acs.jmedchem.0c01023
162673695 183172 0 None -42 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(=O)Nc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4795529 183172 0 None -42 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 347 6 1 3 5.3 CCCCCn1nc(C(=O)Nc2ccc(Cl)cc2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
162623029 183186 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 399 5 2 5 3.6 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(OC(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4795667 183186 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 399 5 2 5 3.6 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(OC(F)(F)F)cc2)n1 10.1021/acs.jmedchem.0c01023
162675834 183265 0 None -25 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccn2)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4796542 183265 0 None -25 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 316 4 2 5 2.1 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccn2)n1 10.1021/acs.jmedchem.0c01023
162676075 183300 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 418 4 2 5 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncc(C(F)(F)F)cc2Cl)n1 10.1021/acs.jmedchem.0c01023
CHEMBL4797039 183300 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 418 4 2 5 3.7 CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncc(C(F)(F)F)cc2Cl)n1 10.1021/acs.jmedchem.0c01023
162676388 183379 0 None -478 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 281 5 2 4 2.1 CCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4797941 183379 0 None -478 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 281 5 2 4 2.1 CCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
162675814 183447 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 297 6 2 5 1.3 COCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4798902 183447 0 None 1 2 Human 4.0 pEC50 = 4 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 297 6 2 5 1.3 COCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
57606070 74577 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 455 7 2 5 2.7 CNC(=O)CC[C@@H](CO)N(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
CHEMBL2029737 74577 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
ChEMBL 455 7 2 5 2.7 CNC(=O)CC[C@@H](CO)N(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1 10.1016/j.bmcl.2012.04.128
155535617 172066 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
CHEMBL4472094 172066 1 None -3 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay
ChEMBL 330 8 2 4 2.5 CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21 10.1039/d1md00242b
60155823 76996 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 340 5 2 1 4.7 CCc1c(C(=O)NCCc2ccc(C)cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b00579
CHEMBL2071064 76996 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 340 5 2 1 4.7 CCc1c(C(=O)NCCc2ccc(C)cc2)[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.5b00579
164624856 185538 0 None -5 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 337 7 0 4 4.5 CCCCCc1cc(OC)c2cc(Cc3ccccn3)c(=O)oc2c1 10.1016/j.ejmech.2021.113354
CHEMBL4862930 185538 0 None -5 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay
ChEMBL 337 7 0 4 4.5 CCCCCc1cc(OC)c2cc(Cc3ccccn3)c(=O)oc2c1 10.1016/j.ejmech.2021.113354
67953300 115693 0 None -1288 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 291 4 1 4 2.8 CC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2CC2CC2)no1 10.1016/j.bmcl.2014.12.019
CHEMBL3353867 115693 0 None -1288 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins
ChEMBL 291 4 1 4 2.8 CC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2CC2CC2)no1 10.1016/j.bmcl.2014.12.019
118324104 150426 0 None - 1 Human 6.0 pEC50 = 6 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 572 10 3 4 8.0 O=C(O)CCCOc1ccc(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)cc1 nan
CHEMBL3953885 150426 0 None - 1 Human 6.0 pEC50 = 6 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 572 10 3 4 8.0 O=C(O)CCCOc1ccc(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)cc1 nan
118323970 147443 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 722 12 2 6 7.7 CC(=O)NCCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
CHEMBL3930097 147443 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 722 12 2 6 7.7 CC(=O)NCCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
71087679 159978 0 None -25 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 389 7 2 5 2.4 CNC(=O)[C@@H](NC(=O)c1ccc(C2CC2)c(OCC2CCCO2)n1)C(C)(C)C nan
CHEMBL4107610 159978 0 None -25 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 389 7 2 5 2.4 CNC(=O)[C@@H](NC(=O)c1ccc(C2CC2)c(OCC2CCCO2)n1)C(C)(C)C nan
57403187 70641 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 427 5 0 3 5.3 C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950331 70641 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 427 5 0 3 5.3 C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(Cc1ccccc1)CC2 10.1016/j.bmcl.2011.12.124
11856745 70650 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 423 4 0 4 4.5 CCCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2 10.1016/j.bmcl.2011.12.124
CHEMBL1950341 70650 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
ChEMBL 423 4 0 4 4.5 CCCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2 10.1016/j.bmcl.2011.12.124
118324125 144218 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 605 8 2 5 7.6 CC(C)(C)OC(=O)CCN1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
CHEMBL3904458 144218 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 605 8 2 5 7.6 CC(C)(C)OC(=O)CCN1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1 nan
162677250 183531 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 319 6 1 3 4.4 CCCCCn1nc(C(=O)NC2CCCCC2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
CHEMBL4799912 183531 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay
ChEMBL 319 6 1 3 4.4 CCCCCn1nc(C(=O)NC2CCCCC2)cc1C(C)(C)C 10.1021/acs.jmedchem.0c01023
10141893 376 56 None -72 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 503 5 0 5 4.9 CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O 10.1016/j.bmcl.2014.11.003
3316 376 56 None -72 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 503 5 0 5 4.9 CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O 10.1016/j.bmcl.2014.11.003
CHEMBL408430 376 56 None -72 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 503 5 0 5 4.9 CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O 10.1016/j.bmcl.2014.11.003
72948611 172914 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assayAgonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay
ChEMBL 359 6 0 2 6.4 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2cccc(F)c21 10.1021/acs.jmedchem.6b00516
CHEMBL4516360 172914 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assayAgonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay
ChEMBL 359 6 0 2 6.4 CCCCCn1cc(C(=O)c2cccc3ccccc23)c2cccc(F)c21 10.1021/acs.jmedchem.6b00516
168297756 192496 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assayAgonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay
ChEMBL 364 8 2 4 2.7 CCCCn1cc(C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c2cccnc21 10.1039/d1md00242b
CHEMBL5209051 192496 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assayAgonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay
ChEMBL 364 8 2 4 2.7 CCCCn1cc(C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c2cccnc21 10.1039/d1md00242b
118720565 115952 0 None -87 3 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 115952 0 None -87 3 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 85043 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 404 4 2 1 6.6 O=C(Nc1ccc(Cl)cc1)NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm0503906
CHEMBL224113 85043 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
ChEMBL 404 4 2 1 6.6 O=C(Nc1ccc(Cl)cc1)NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm0503906
53324282 57062 0 None -104 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 351 4 1 2 5.4 Clc1cccc(-c2c[nH]c(-c3cccc(CN4CCCCC4)c3)n2)c1 10.1016/j.bmcl.2010.11.044
CHEMBL1644739 57062 0 None -104 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 351 4 1 2 5.4 Clc1cccc(-c2c[nH]c(-c3cccc(CN4CCCCC4)c3)n2)c1 10.1016/j.bmcl.2010.11.044
44828492 2963 76 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 409 6 2 2 5.3 CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1 10.1021/acs.jmedchem.5b00579
7851 2963 76 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 409 6 2 2 5.3 CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1 10.1021/acs.jmedchem.5b00579
CHEMBL1553629 2963 76 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
ChEMBL 409 6 2 2 5.3 CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1 10.1021/acs.jmedchem.5b00579
71093593 142851 0 None -12 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 356 7 1 6 3.1 Cc1nc(C(C)(C)NC(=O)c2ccc(C3CC3)c(OCC3CC3)n2)no1 nan
CHEMBL3893213 142851 0 None -12 2 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.
ChEMBL 356 7 1 6 3.1 Cc1nc(C(C)(C)NC(=O)c2ccc(C3CC3)c(OCC3CC3)n2)no1 nan
118323971 145660 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 10.1021/acs.jmedchem.8b01467
CHEMBL3915918 145660 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 10.1021/acs.jmedchem.8b01467
118323971 145660 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
CHEMBL3915918 145660 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.
ChEMBL 709 12 2 6 8.1 O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12 nan
22475020 96003 19 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.1021/jm701487t
CHEMBL259656 96003 19 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 491 3 0 4 5.4 O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1 10.1021/jm701487t
22475055 159543 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 513 4 0 5 4.1 O=S(=O)(c1cc2c(cc1F)OC(c1ccc(F)cc1F)(c1ccc(F)cc1F)O2)N1CCOCC1 10.1021/jm701487t
CHEMBL410247 159543 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level
ChEMBL 513 4 0 5 4.1 O=S(=O)(c1cc2c(cc1F)OC(c1ccc(F)cc1F)(c1ccc(F)cc1F