Table 2.
Characterizing selectivity of Sch.414319 for the human cannabinoid CB2 receptor
| ID | Name | Type | % lnhbt @ 10 μM | Protocol reference |
|---|---|---|---|---|
| 10730 | Angiotensin-converting enzyme | Enz | 8 | Bunning P et al. Biochemistry. 22:103, 1983 |
| 10800 | Protease calpain | Enz | 19 | Murachi T et al. Adv Enzyme Regul. 19: 407, 1980 |
| 11200 | Carbonic anhydrase | Enz | 3 | Eveloff J et al. Biochem Pharmacol. 28: 1434, 1979 |
| 11250 | Protease cathepsin G | Enz | 1 | Mehdi S et al. Biochem Biophys Res Commun. 166: 595, 1990 |
| 11300 | Choline acetyltranferase | Enz | 3 | Maderdrut JL. Neurochem Res. 20: 69, 1995 |
| 11501 | Cyclooxygenase COX-1 | Enz | −14 | Warner TD et al. Proc Natl Acad Sci USA. 96: 7563, 1999 |
| 11601 | Cyclooxygenase COX-2 | Enz | 18 | Warner TD et al. Proc Natl Acad Sci USA. 96(13): 7563, 1999 |
| 12100 | Myeloperoxidase | Enz | −7 | Syensson BE. Biochem J. 242: 673, 1987 |
| 12400 | HMG-CoA reductase | Enz | −1 | Kubo M and Strott CA. Endocrinology. 120: 214, 1987 |
| 12800 | Leukotriene A4 hydrolase | Enz | 20 | laumi T et al. Biochem Biophys Res Commun. 135: 139, 1986 |
| 13200 | Leukotriene C4 synthetase | Enz | −11 | Bach MK et al. Biochem Pharmacol. 34: 2695, 1985 |
| 13400 | Lipid peroxidase | Enz | 20 | Mansuy D et al. Biochem Biophys Res Commun. 135: 1015, 1986 |
| 13800 | Lipoxygenase 15-LO | Enz | 2 | Averbach BJ et al. Anal Biochem. 201: 375, 1992 |
| 14000 | Monoamine oxidase MAOA | Enz | 1 | Medvedev AE et al. Biochem Pharmacol. 47: 303, 1994 |
| 14010 | Monoamine oxidase MAOB | Enz | −11 | Egashira T et al. Biochem Pharmacol. 25: 2583, 1976 |
| 14200 | Nitric oxide sythase constitutive (cNOS) | Enz | 3 | Lowenstein CJ and Snyder SH. Cell. 70: 705, 1992 |
| 14400 | Nitric oxide sythase inducible (iNOS) | Enz | 3 | Nathan C. FASEB J. 6: 3051, 1992 |
| 14600 | Phosphodiesterase PDE1 | Enz | 65 | Nicholsen CD et al. Trends Pharmacol Sci. 12: 19, 1991 |
| 14800 | Phosphodiesterase PDE2 | Enz | 25 | Hidaka H and Asano T. Biochem Biophys Acta. 429: 485, 1976 |
| 15200 | Phosphodiesterase PDE3 | Enz | 12 | Nicholsen CD et al. Trends Pharmacol Sci. 12: 19, 1991 |
| 15400 | Phosphodiesterase PDE4 | Enz | 27 | Cortijo J et al. Br J Pharmacol. 108: 562, 1993 |
| 15600 | Phosphodiesterase PDE5 | Enz | 5 | Hidaka H and Asano T. Biochem Biophys Acta. 429: 485, 1976 |
| 16000 | Phospholipase PLA2-1 | Enz | 19 | Katsumata M et al. Anal Biochem. 154: 676, 1986 |
| 16400 | Protease neutral endopeptidase | Enz | −2 | Erdos EG and Skidgel RA. FASEB J. 3: 145, 1989 |
| 16600 | Protease elastase | Enz | 1 | Baugh J and Travis J Biochemistry. 15(4): 836, 1976 |
| 16800 | Protein kinase II, Ca2+/calmodulin-dep. | Enz | 18 | Lai Y et al. Proc Natl Acad Sci USA. 83: 4253, 1986. |
| 17000 | EGF receptor tyrosine kinase | Enz | −9 | Geissler JF et al. J Biol Chem. 265: 22255, 1990 |
| 17100 | ERK1 serine/threonine kinase | Enz | 10 | Dudley DT et al. Proc Natl Acad Sci USA. 32: 7686, 1995 |
| 17200 | Fya (p59fya) tyrosine kinase | Enz | −6 | Appleby MW et al. Cell. 70: 751, 1992 |
| 17400 | HER2 tyrosine kinase | Enz | 12 | Bargmann CI et al. Cell. 45: 649, 1986 |
| 17600 | Lck (p56lck) tyrosine | Enz | 6 | Caron L et al. Mol Cell Biol. 12: 2720, 1992 |
| 17700 | PKA non-selective | Enz | 5 | Quick J et al. Biochem Biophys Res Commun. 187: 657, 1992 |
| 17800 | Protein kinase C, non-selective | Enz | 1 | Jeng AY et al. Cancer Res. 46: 1966, 1986 |
| 18001 | Protein Kinase C alpha | Enz | 1 | Tamaki T et al. Biochem Biophys Res Commun. 135: 397, 1986 |
| 18200 | Protein kinase C- (I and II) | Enz | 17 | Woodgett JR and Hunter T. J Biol Chem. 262: 4836, 1987 |
| 18400 | Protein kinase C- | Enz | −14 | Woodgett JR and Hunter T. J Biol Chem. 262: 4836, 1987 |
| 18600 | Calcineurin PP2B phosphatase | Enz | 5 | Klee CB et al. Methods Enzymol. 102: 227, 1983 |
| 19000 | CD45 tyrosine phosphatase | Enz | 5 | Zhang ZY et al. Proc Natl Acad Sci USA. 90: 4446, 1993 |
| 19200 | PTP1B tyrosine phosphatase | Enz | −2 | Wiener JR et al. J Natl Cancer last. 86: 372, 1994 |
| 19220 | PTP1C tyrosine phosphatase | Enz | 13 | D'Ambrosio D et al. Science. 268: 293, 1995 |
| 19300 | T-cell tyrosine phosphatase | Enz | −2 | Yakura H Crit Rev Immunol. 14: 311, 1994 |
| 19350 | Free radical scavenger, SOD mimetic | Enz | 29 | Sun Y et al. Clin Chem. 34: 467, 1988 |
| 19400 | Thromboxane synthetase | Enz | 48 | Fiddler Gl and Lumley P. Circulation. 81: 169, 1990 |
| 19500 | Tyrosine hydroxylase | Enz | 19 | Roskoshi R Jr et al. J Biochem. 218: 363, 1993 |
| 19800 | Xanthine oxidase | Enz | −1 | Hatano T et al. Chem Pharm Bull. 38: 1224, 1990 |
| 20031 | Adenosine A1 | Bind | 22 | Libert F et al. Biochem Biophys Res Commun. 187: 919, 1992 |
| 20061 | Adenosine A2A | Bind | 47 | Jarvis MF et al. J Pharmacol Exp Ther. 251: 888, 1989 |
| 20071 | Adenosine A3 | Bind | 46 | Olah ME et al. Mol Pharmacol. 45: 978, 1994 |
| 20080 | Adenosine A2B | Bind | 38 | Brackett LE and Daly JW. Biochem Pharmacol. 47: 801, 1994 |
| 20340 | Adrenergic-1D | Bind | 27 | Kenny BA et al. Br. J Pharmacol. 115: 981, 1995 |
| 20362 | Adrenergic-2A | Bind | 3 | Uhlen S et al. J Pharmacol Exp Ther. 271: 1558, 1994 |
| 20380 | Adrenergic-2C | Bind | 13 | Uhlen S et al. J Pharmacol Exp Ther. 271: 1558, 1994 |
| 20401 | Adrenergic 1 | Bind | 3 | Feve B et al. Proc Natl Acad Sci USA. 91: 5677, 1994 |
| 20411 | Adrenergic-2 | Bind | −5 | McCrea KE and Hill SJ. Br. J Pharmacol. 110: 619, 1993 |
| 20420 | Adrenergic-3 | Bind | 36 | Feve B et al. Proc Natl Acad Sci USA. 91: 5677, 1994 |
| 20441 | Adrenergic norepinephrine transporter | Bind | 38 | Galli A et al. J Exp Biol. 198: 2197, 1995 |
| 21001 | Angiotensin AT1 | Bind | 22 | Dudley DT et al. Mol Pharmacol. 38: 370, 1990 |
| 21011 | Angiotensin AT2 | Bind | 7 | Whitebread SE et al. Biochem Biophys Res Commun. 181: 1365, 1991 |
| 21261 | Bradykinin B2 | Bind | 10 | Eggerickx D et al. Biochem Biophys Res Commun. 187(3): 1306, 1992 |
| 21361 | Calcitonin | Bind | 9 | Findlay DM et al. Cancer Res. 40: 1311, 1980 |
| 21401 | Calcitonin gene-related peptide (CGRP) | Bind | −5 | Zimmermann U et al. Peptide. 16(3): 421, 1995 |
| 21450 | Calcium channel type l, benzothiazepine | Bind | 69 | Schoemaker H and Langer SZ. Eur J Pharmacol. 111: 273, 1985 |
| 21460 | Calcium channel type l, dihydropyridine | Bind | 92 | Gould RJ et al. Proc Natl Acad Sci USA. 79: 3656, 1982 |
| 21500 | Calcium channel type l, phenylalkylamine | Bind | 72 | Reynolds IJ et al. J Pharmacol Exp Ther. 237: 731, 1986 |
| 21600 | Calcium channel type N | Bind | −1 | Moresco RM et al. Neurobiol Aging. 11(4): 433, 1990 |
| 21701 | Cannabinoid CB1 | Bind | 10 | Felder CC et al. Mol Pharmacol. 48: 443, 1995 |
| 21710 | Cannabinoid CB2 | Bind | 85 | Munro S et al. Nature. 365: 61, 1993 |
| 21801 | Cholecystokinin CCKA | Bind | 10 | Jensen RT et al. Ann N Y Acad Sci. 713: 88, 1994 |
| 21811 | Cholecystokinin CCKB | Bind | 55 | Jensen RT et al. Ann N Y Acad Sci. 713: 88, 1994 |
| 21850 | Dopamine D1 | Bind | −1 | Dearry A et al. Nature. 347: 72, 1990 |
| 21860 | Dopamine D2L | Bind | 26 | Hayes G et al. Mol Endocrinol. 6: 920, 1992 |
| 21870 | Dopamine D2S | Bind | 18 | Grandy DK et al. Proc Natl Acad Sci USA. 86: 9762, 1989 |
| 21880 | Dopamine D3 | Bind | 30 | Sokoloff P et al. Nature. 347: 146, 1990 |
| 21890 | Dopamine D4-2 | Bind | 11 | Van Tol HHM et al. Nature. 358: 149, 1992 |
| 22000 | Dopamine D4-4 | Bind | −6 | Van Tol HHM et al. Nature. 350: 610, 1991 |
| 22010 | Dopamine D4-7 | Bind | −8 | Van Tol HHM et al. Nature. 358: 149, 1992 |
| 22020 | Dopamine D5 | Bind | 20 | Sunahara RK et al. Nature. 350: 614, 1991 |
| 22032 | Dopamine transporter | Bind | 36 | Gu H et al. J. Biol Chem. 269: 7124, 1994 |
| 22410 | Endothelin ETB | Bind | −14 | Mihara S et al. J Pharmacol Exp Ther. 268: 1122, 1994 |
| 22550 | Epidermal growth factor (EGF) | Bind | 6 | Dittadi R et al. Clin Chem. 36: 849, 1990 |
| 22601 | Estrogen ER | Bind | 8 | Obourn JD et al. Biochem. 32: 6229, 1993 |
| 23131 | Galanin | Bind | −4 | Heullet E et al. Eur J Pharmacol. 269: 139, 1994 |
| 23170 | Glucagon-like peptide-1 (GLP-1) | Bind | 14 | Dillon JS et al. Endocrinology. 133: 1907, 1993 |
| 23201 | Glucocorticoid | Bind | 14 | Cidlowski JA and Cidlowski NB. Endocrinology. 109: 1975, 1981 |
| 23350 | Histamine H1, central | Bind | 4 | Hill SJ et al. J Neurochem. 31: 997, 1978 |
| 23360 | Histamine H1, peripheral | Bind | −14 | Dini S et al. Agents Actions. 33: 181, 1991 |
| 23370 | Histamine H2 | Bind | 23 | Traiffort E et al. Eur J Pharmacol. 207: 143, 1991 |
| 23380 | Histamine H3 | Bind | 11 | West RE et al. Mol Pharmacol. 38: 610, 1990 |
| 24410 | Laterleukin IL-6 | Bind | 9 | Cornfield LJ and sills MA. Eur J Pharmacol. 202: 113, 1991 |
| 24430 | Chemokine CXCR1/2 (IL-8, non-selective) | Bind | −17 | Moser B et al. J Biol Chem. 266: 10666, 1991 |
| 24440 | Chemokine CXCR1 | Bind | 3 | Ahuja SK et al. J Biol Chem. 271: 20545, 1996 |
| 24450 | Chemokine CXCR2 | Bind | 8 | Ahuja SK et al. J Biol Chem. 271: 20545, 1996 |
| 25051 | Leukotriene B4 | Bind | −10 | Winkler JD et al. J Pharmacol Exp Ther. 246: 204, 1988 |
| 25060 | Leukotriene D4 | Bind | 6 | Mong S et al. Eur J Pharmacol. 102: 1, 1984 |
| 25260 | Muscarinic M1 | Bind | −23 | Buckley NJ et al. Mol Pharmacol. 35: 469, 1989 |
| 25270 | Muscarinic M2 | Bind | 2 | Buckley NJ et al. Mol Pharmacol. 35: 469, 1989 |
| 25280 | Muscarinic M3 | Bind | −7 | Buckley NJ et al. Mol Pharmacol. 35: 469, 1989 |
| 25290 | Muscarinic M4 | Bind | −5 | Buckley NJ et al. Mol Pharmacol. 35: 469, 1989 |
| 25300 | Muscarinic M5 | Bind | −18 | Buckley NJ et al. Mol Pharmacol. 35: 469, 1989 |
| 25551 | Tachykinin NK1 | Bind | 14 | Patacchini R and Maggi CA. Arch Int Pharmacodyn Ther. 329: 161, 1995 |
| 25560 | Tachykinin NK2 | Bind | 1 | Patacchini R and Maggi CA. Arch Int Pharmacodyn Ther. 329: 161, 1995 |
| 25570 | Tachykinin NK3 | Bind | 0 | Patacchini R and Maggi CA. Arch Int Pharmacodyn Ther. 329: 161, 1995 |
| 25700 | Neuropeptide Y1 | Bind | 22 | Fuhlendorff J et al. Proc Natl Acad Sci USA. 87: 182, 1990 |
| 25711 | Neuropeptide Y2 | Bind | −11 | Rose PM et al. J Biol Chem. 270(39): 22661, 1995 |
| 26011 | Opiate delta | Bind | 9 | Simonin F et al. Mol Pharmacol. 46: 1015, 1994 |
| 26021 | Opiate- | Bind | 8 | Simonin F et al. Proc Natl Acad Sci USA. 92(15): 7006, 1995 |
| 26041 | Opiate- | Bind | 23 | Wang JB et al. FEBS Lett. 338: 217, 1994 |
| 26060 | Orphanin (ORL1) | Bind | 7 | Ardati A et al. Mol Pharmacol. 51: 816, 1997 |
| 26330 | Potassium channel [KA] | Bind | 23 | Rehm H and Laadunski M. Proc Natl Acad Sci USA. 85: 4919, 1988 |
| 26370 | Potassium channel [KV] | Bind | −5 | Vazquez J et al. J Biol Chem. 264: 20902, 1989 |
| 26560 | Potassium channel [SKCA] | Bind | 2 | Mourre C et al. Brain Res. 382: 239, 1986 |
| 26670 | Purinergic P2X | Bind | 7 | Ziganshin AU et al. Br J Pharmacol. 110: 1431, 1993 |
| 27111 | Serotonin 5-HT1A | Bind | 2 | Martin GR and Humphrey PPA. Neuropharmacol. 33: 261, 1994 |
| 27130 | Serotonin 5-HT1D | Bind | −2 | Domenech T et al. Naunyn Schmiedebergs Arch Pharmacol. 356: 328, 1997 |
| 27165 | Serotonin 5-HT2A | Bind | 31 | Saucier C and Albert PR. J Neurochem. 68: 1998, 1997 |
| 27210 | Serotonin 5-HT5A | Bind | 21 | Rees S et al. FEBS Lett. 355: 242, 1994 |
| 27220 | Serotonin 5-HT6 | Bind | 54 | Monsma FJ Jr et al. Mol Pharmacol. 43: 320, 1993 |
| 27230 | Serotonin 5-HT7 | Bind | 28 | Roth BL et al. J Pharmacol Exp Ther. 268: 1403, 1994 |
| 27402 | Serotonin transporter | Bind | −5 | Gu H et al. J Biol Chem. 269: 7124, 1994 |
| 27830 | Sigma, non-selective | Bind | 70 | Weber E et al. Proc Natl Acad Sci USA. 83: 8784, 1986 |
| 28550 | Thromboxane A2 [TXA2] | Bind | 59 | Hedberg A et al. J Pharmacol Exp Ther. 245: 786, 1988 |
| 28631 | Tumor hecrosis factor, non-selective | Bind | 11 | Baglioni C et al. J Biol Chem. 260: 13395, 1985 |
| 28680 | Vascular endothelinal growth factor | Bind | 13 | Gitay-Goren H et al. J Biol Chem. 271: 5519, 1996 |
| 28701 | Vasoactive intestinal peptide VIP1 | Bind | −12 | Couvineau A et al. Biochem J. 231: 139, 1985 |
| 28751 | Vasopressia VIA | Bind | 18 | Thibonnier M et al. J Biol Chem. 269: 3304, 1994 |
| 30500 | Adhesion, fibronectin-mediated | Cell | 5.9 | Nowlin D et al. J Biol Chem. 268: 20351, 1993 |
| 30510 | Adhesion, ICAM-1 mediated | Cell | −4.3 | Cobb RR et al. Biochem Biophys Res Commun. 185: 1022, 1992 |
| 30750 | Adhesion, VCAM-1-mediated antagonist | Cell | 26.3 | Stoltenborg JK et al. J Immunol Methods. 175: 59, 1994. |
Abbreviations: Bind, specific binding; EGF, epidermal growth factor; Enz, enzymatic activity; ERK1, extracellular signal-regulated kinase 1; HMG, 3-hydroxy-3-methyl-glutaryl-CoA reductase; PKA, protein kinase A; ICAM, intercellular adhesion molecule; SOD, superoxide dismutase; VCAM, vascular cell adhesion molecule.
The ability of Sch.414319 to affect the biochemical activity of selected assays is presented. Assay results are presented as the percent inhibition of specific binding (Bind), enzymatic activity (Enz) or cellular activity (Cell) according to experimental procedures listed in the references provided.