ChEMBL ligand: CHEMBL307696 (HU-210)
CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] There should be some charts here, you may need to enable JavaScript!
CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] There should be some charts here, you may need to enable JavaScript!
GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6] There should be some charts here, you may need to enable JavaScript!
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415] There should be some charts here, you may need to enable JavaScript!
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] There should be some charts here, you may need to enable JavaScript!
glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311] There should be some charts here, you may need to enable JavaScript!

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 [3H]SR141716A from human CB1 receptor	B	7.73	pKi	18.6	nM	Ki	J Med Chem (2006) 49: 872-882 [PMID:16451053]
ChEMBL	Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis	B	8.02	pKi	9.55	nM	Ki	Medchemcomm (2017) 8: 1697-1705 [PMID:30108881]
ChEMBL	Competition Binding Assay: The Kd of CP 55,940 in the isolated CB1 and CB2 receptor expressing membranes was previously determined to be 2.3 nM and 1.5 nM, respectively (see Pertwee, R. G. Current Medicinal Chemistry 6 635-664 (1999)). Competition binding assays at 2.5 nM [3H]-CP 55,940 (PerkinElmer) were carried out to determine the K1 values for tested compounds. Membranes (5-10 μg) were incubated with radioligand and a range of concentrations of test compounds in binding buffer (50 mM Tris pH 7.4, 5 mM MgCl2, 1 mM EDTA) with 0.5% (w/v) bovine serum albumin (BSA) (ICP Bio, New Zealand), at 30° C. for 60 min. Stock solutions of putative cannabinoid ligands were prepared in dimethyl sulfoxide to a concentration of 10 mM. Six different final concentrations of compounds were used ranging from 50 μM to 0.1 nM. Non-specific binding was determined in the presence of 1 μM non-radioactive CP 55,940 (Tocris Cookson). Assays were terminated by addition of 2 ml ice cold binding buffer and filtration through GF/C filters (Whatman) pre-soaked in cold binding buffer, followed by two washes in the same buffer.	B	8.53	pKi	2.94	nM	Ki	US-9365534-B2. Arylated camphenes, processes for their preparation and uses thereof (2016)
ChEMBL	Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting	B	8.82	pKi	1.5	nM	Ki	Eur J Med Chem (2009) 44: 593-608 [PMID:18511157]
ChEMBL	Binding affinity to human CB1 receptor	B	9.14	pKi	0.73	nM	Ki	J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells	B	9.74	pKi	0.18	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
GtoPdb	-	-	10.2	pKi	-	-	-	Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]
ChEMBL	Binding affinity to CB1 receptor	B	10.22	pKi	0.06	nM	Ki	J Med Chem (2011) 54: 5265-5269 [PMID:21675776]
ChEMBL	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry	F	7.4	pEC50	40	nM	EC50	J Med Chem (2009) 52: 5785-5788 [PMID:19743867]
ChEMBL	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	F	9.22	pEC50	0.6	nM	EC50	J Med Chem (2006) 49: 872-882 [PMID:16451053]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL	Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum	B	8.56	pKi	2.75	nM	Ki	J Med Chem (2006) 49: 872-882 [PMID:16451053]
ChEMBL	Binding affinity for the Cannabinoid receptor using [3H]CP-55940 as radioligand	B	9.14	pKi	0.73	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2223-2226 [PMID:9873517]
ChEMBL	Binding affinity to rat CB1 receptor	B	9.15	pKi	0.7	nM	Ki	J Med Chem (2016) 59: 6903-6919 [PMID:27367336]
ChEMBL	Displacement of [3H]CP-55940 binding to Cannabinoid receptor 1 in rat brain membranes	B	9.64	pKi	0.23	nM	Ki	J Med Chem (1998) 41: 4207-4215 [PMID:9784095]
ChEMBL	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	F	8.3	pEC50	5.01	nM	EC50	J Med Chem (2006) 49: 554-566 [PMID:16420041]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem (2013) 21: 7481-7498 [PMID:24139843]
ChEMBL	Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB2 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis	B	8.01	pKi	9.78	nM	Ki	Medchemcomm (2017) 8: 1697-1705 [PMID:30108881]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2006) 49: 70-79 [PMID:16392793]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant cannabinoid CB2 receptor expressed in CHO-K1 cells	B	8.58	pKi	2.66	nM	Ki	Bioorg Med Chem Lett (2011) 21: 5859-5862 [PMID:21855337]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2016) 59: 6903-6919 [PMID:27367336]
ChEMBL	Binding affinity to human CB2 receptor	B	9.66	pKi	0.22	nM	Ki	J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
GtoPdb	-	-	9.8	pKi	-	-	-	Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; J Med Chem (1997) 40: 3228-33 [PMID:9379442]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes	B	9.82	pKi	0.15	nM	Ki	Bioorg Med Chem (2014) 22: 4770-4783 [PMID:25065940]
ChEMBL	Binding affinity to human recombinant CB2 receptor expressed in african green monkey COS cells by radioligand binding assay	B	9.82	pKi	0.15	nM	Ki	J Med Chem (2009) 52: 2506-2514 [PMID:19331413]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells	B	9.82	pKi	0.15	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in HEK cell membrane	B	9.82	pKi	0.15	nM	Ki	Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793]
ChEMBL	Effect on [35S]GTP-gamma-S binding to human CB2 receptor	F	8.39	pEC50	4.1	nM	EC50	J Med Chem (2006) 49: 70-79 [PMID:16392793]
ChEMBL	Agonist activity at human recombinant CB2 receptor expressed in Saccharomyces cerevisiae cells	F	8.52	pEC50	3	nM	EC50	J Med Chem (2007) 50: 2597-2600 [PMID:17477516]
ChEMBL	Agonist activity at human recombinant cannabinoid CB2 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry	F	8.52	pEC50	3	nM	EC50	J Med Chem (2009) 52: 5785-5788 [PMID:19743867]
ChEMBL	Agonist activity at human CB2 receptor expressed in yeast cells assessed as degradation of FDGlu to fluorescein after 24 hrs	F	8.6	pEC50	2.51	nM	EC50	Bioorg Med Chem Lett (2009) 19: 259-263 [PMID:19010671]
ChEMBL	Agonist activity at human CB2 receptor transfected in CHO cell membranes after 90 mins by [35S]-GTPgammaS assay	F	9.2	pEC50	0.63	nM	EC50	Eur J Med Chem (2015) 97: 10-18 [PMID:25935384]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL	Binding affinity to mouse CB2 receptor	B	9.7	pKi	0.2	nM	Ki	J Med Chem (2016) 59: 6903-6919 [PMID:27367336]
GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6]
GtoPdb	-	-	7.59	pEC50	26	nM	EC50	Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302]
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
GtoPdb	-	-	6.6	pEC50	270	nM	EC50
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb	-	-	7	pIC50	90	nM	IC50
glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311]
GtoPdb	-	-	7.3	pIC50	50	nM	IC50

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]