SR144528 [Ligand Id: 751] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL381791
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins by Cheng-Prusoff equation analysis B 3.93 pKi 116800 nM Ki Eur J Med Chem (2019) 178: 243-258 [PMID:31185414]
ChEMBL Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB1 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method B 5.25 pKi 5628 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]CP55,940 from human CB1 receptor B 5.77 pKi 1698.24 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]CP55,940 from human CB1 receptor B 5.77 pKi 1698.2 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay B 6.16 pKi 687 nM Ki J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method B 6.16 pKi 687 nM Ki J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Displacement of [3H]-CP 55,940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting method B 6.4 pKi 400 nM Ki MedChemComm (2015) 6: 1978-1986
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor transfected in CHO cell membranes by liquid scintillation counting analysis B 6.4 pKi 400 nM Ki Eur. J. Med. Chem. (2015) 101: 651-667 [PMID:26209834]
ChEMBL Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 90 mins B 6.6 pKi 254 nM Ki J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB1 receptor expressed in human HEK293 cell membrane after 90 mins B 6.92 pKi 121.2 nM Ki Eur. J. Med. Chem. (2012) 52: 284-294 [PMID:22483967]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis B 8.7 pKi 2 nM Ki Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method B 6.1 pIC50 794.33 nM IC50 J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins by Cheng-Prusoff equation analysis B 5.74 pKi 1820 nM Ki Eur J Med Chem (2019) 178: 243-258 [PMID:31185414]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis B 6.93 pKi 117 nM Ki Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB2 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method B 7.29 pKi 51 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]-CP55940 from human recombinant cannabinoid CB2 receptor expressed in human HEK cells by radioligand binding assay B 7.71 pKi 19.7 nM Ki J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method B 7.71 pKi 19.7 nM Ki J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Displacement of [3H]CP55,940 from human CB2 receptor B 7.88 pKi 13.2 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]CP55,940 from human CB2 receptor B 7.88 pKi 13.18 nM Ki Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 90 mins B 8.25 pKi 5.6 nM Ki J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB2 receptor expressed in human HEK293 cell membrane after 90 mins B 8.36 pKi 4.35 nM Ki Eur. J. Med. Chem. (2012) 52: 284-294 [PMID:22483967]
ChEMBL Displacement of [3H]CP-55,940 from human CB2 receptor after 1 hr by competitive binding assay B 8.65 pKi 2.23 nM Ki J. Med. Chem. (2013) 56: 6593-6612 [PMID:23855811]
ChEMBL Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay B 8.74 pKi 1.82 nM Ki Eur J Med Chem (2016) 122: 619-634 [PMID:27448919]
ChEMBL Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes measured after 90 mins B 8.74 pKi 1.8 nM Ki Eur J Med Chem (2019) 161: 239-251 [PMID:30359820]
GtoPdb - - 9.2 pKi 0.63 nM Ki Br J Pharmacol (1999) 126: 665-672 [PMID:10188977];
J Pharmacol Exp Ther (1998) 284: 644-50 [PMID:9454810]
ChEMBL Displacement of [3H]-CP 55,940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting method B 9.22 pKi 0.6 nM Ki MedChemComm (2015) 6: 1978-1986
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor transfected in CHO cell membranes by liquid scintillation counting analysis B 9.22 pKi 0.6 nM Ki Eur. J. Med. Chem. (2015) 101: 651-667 [PMID:26209834]
ChEMBL Binding affinity to human CB2 receptor expressed in CHO cells B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2013) 56: 6593-6612 [PMID:23855811]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis B 9.51 pKi 0.31 nM Ki Eur. J. Med. Chem. (2015) 101: 651-667 [PMID:26209834]
ChEMBL Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins B 5.15 pIC50 7160 nM IC50 Eur J Med Chem (2019) 178: 243-258 [PMID:31185414]
ChEMBL Inverse agonist activity at N-terminal HA-tagged human CB2 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as increase in forskolin-stimulated cAMP level by BRET assay F 6.12 pIC50 760 nM IC50 Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay B 7.02 pIC50 96.2 nM IC50 Eur J Med Chem (2017) 127: 398-412 [PMID:28088085]
ChEMBL Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method B 7.7 pIC50 19.95 nM IC50 J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL Agonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as increase of beta-arrestin recruitment by Tango assay B 5.87 pEC50 1360 nM EC50 Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL Antagonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assay B 7.39 pEC50 41 nM EC50 Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb = 4.21+/-1.16 nM) F 7.63 pEC50 23.31 nM EC50 J. Med. Chem. (2013) 56: 6593-6612 [PMID:23855811]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]