BindingDB BDBM21278 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide::Acomplia::CHEMBL111::CHEMBL558598::RIMONABANT HYDROCHLORIDE::Rimonabant::SR 141716A::SR141716::SR141716A::[3H]Rimonabant::[3H]SR141716A

BDBM21278 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide::Acomplia::CHEMBL111::CHEMBL558598::RIMONABANT HYDROCHLORIDE::Rimonabant::SR 141716A::SR141716::SR141716A::[3H]Rimonabant::[3H]SR141716A

SMILES Cc1c(nn(c1-c1ccc(Cl)cc1)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1

InChI Key InChIKey=JZCPYUJPEARBJL-UHFFFAOYSA-N

Data 155 KI 79 IC50 10 Kd 24 EC50

PDB links: 1 PDB ID matches this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 24 hits for monomerid = 21278

Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

Ki: 1.80nM ΔG°: -12.1kcal/mole EC50: 1.60nMpH: 7.4 T: 2°CAssay Description:IC50 values for test compounds were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibition c...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 50nMAssay Description:Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP af...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 50nMAssay Description:Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP af...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Rattus norvegicus (rat))
Neurogen

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 0.170nMAssay Description:Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 18.2nMAssay Description:Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP bindingMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 18.2nMAssay Description:Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP bindingMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 5nMAssay Description:Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Cal...More data for this Ligand-Target Pair

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Cannabinoid receptor 2(Homo sapiens (Human))
Corbus Pharmaceuticals

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 3.12E+4nMAssay Description:Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activityMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 240nMAssay Description:Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 15.7nMAssay Description:Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP55940-stimulated Eu-GTP bindingMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Mus musculus (Mouse))
Neuroscienze Pharmaness S.C.A R.L.

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 8.99E+3nMAssay Description:Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contractionMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 0.110nMAssay Description:Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation af...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Rattus norvegicus (rat))
Neurogen

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 5.63E+4nMAssay Description:Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 10.1nMAssay Description:Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 10.1nMAssay Description:Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayMore data for this Ligand-Target Pair

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G-protein coupled receptor 55(Homo sapiens (Human))
University Of Bonn

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 2.01E+3nMAssay Description:Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by ...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 4nMAssay Description:Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 36nMAssay Description:Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 586nMAssay Description:Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after...More data for this Ligand-Target Pair

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Cannabinoid receptor 2(Homo sapiens (Human))
Corbus Pharmaceuticals

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: >1.00E+4nMAssay Description:Inverse agonist activity at human CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins ...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 4.10nMAssay Description:Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins ...More data for this Ligand-Target Pair

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Cannabinoid receptor 2(MOUSE)
Neuroscienze Pharmaness S.C.A R.L.

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 15nMAssay Description:Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-ar...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Homo sapiens (Human))
National Institute Of Mental Health

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 4.10nMAssay Description:Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF ass...More data for this Ligand-Target Pair

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Cannabinoid receptor 1(Rattus norvegicus (rat))
Neurogen

Curated by ChEMBL

PNG

BDBM21278(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl...)

EC50: 3.09E+3nMAssay Description:Agonist activity at rat brain membrane CB1 receptor assessed as stimulation of [35S]GTPgammaS binding incubated for 60 minsMore data for this Ligand-Target Pair

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Filter my 267 hits

Targets 27▿
- Cannabinoid receptor 1 166
- Cannabinoid receptor 2 73
- ATP-binding cassette sub-family C member 4 2
- Potassium voltage-gated channel subfamily H member 2 2
- Bile salt export pump 2
- Multidrug resistance-associated protein 1 1
- Cannabinoid receptor 1 [P221A] 1
- Cannabinoid receptor 1 [T344A] 1
- Cannabinoid receptor 1 [D338A] 1
- Cannabinoid receptor 1 [I218A] 1
- GTP-binding nuclear protein GSP1/CNR1 1
- Cannabinoid receptor 1 [H219A] 1
- CB1 cannabinoid receptor-interacting protein 1 1
- Cannabinoid receptor 1 [R340A] 1
- ATP-binding cassette sub-family C member 3 1
- Cytochrome P450 1A2 1
- ATP-binding cassette sub-family C member 2 1
- Cannabinoid receptor 1 [I339A] 1
- G-protein coupled receptor 55 1
- Cytochrome P450 2C9 1
- GTP-binding nuclear protein GSP2/CNR2 1
- Cannabinoid receptor 1/2 1
- Fatty acid-binding protein, liver 1
- Cytochrome P450 2D6 1
- N-arachidonyl glycine receptor 1
- Cytochrome P450 3A4 1
- Cannabinoid receptor 1 [I341A] 1
Publications 50▿
- J Biol Chem 288: 32449-65 (2013) 9
- Bioorg Med Chem 18: 6377-88 (2010) 7
- J Med Chem 61: 10276-10298 (2018) 4
- Eur J Med Chem 121: 194-208 (2016) 4
- J Med Chem 51: 2439-46 (2008) 4
- Toxicol Sci 136: 216-41 (2013) 4
- J Med Chem 46: 5139-52 (2003) 4
- J Med Chem 53: 7048-60 (2010) 4
- J Med Chem 51: 5608-16 (2008) 4
- Eur J Med Chem 45: 1133-9 (2010) 4
- Bioorg Med Chem Lett 18: 3376-81 (2008) 4
- Bioorg Med Chem Lett 19: 1022-5 (2009) 4
- J Med Chem 59: 6753-6771 (2016) 4
- Bioorg Med Chem Lett 19: 4183-90 (2009) 3
- J Med Chem 49: 5969-87 (2006) 3
- ACS Med Chem Lett 4: 41-5 (2013) 3
- J Med Chem 49: 872-82 (2006) 3
- Bioorg Med Chem Lett 21: 2034-9 (2011) 3
- J Med Chem 51: 5397-412 (2008) 3
- Bioorg Med Chem 26: 4518-4531 (2018) 3
- J Med Chem 65: 2374-2387 (2022) 3
- J Med Chem 51: 3526-39 (2008) 3
- J Med Chem 45: 2708-19 (2002) 3
- Bioorg Med Chem 16: 4035-51 (2008) 3
- Bioorg Med Chem Lett 19: 6632-6 (2009) 3
- Eur J Med Chem 74: 73-84 (2014) 3
- Bioorg Med Chem 24: 1063-70 (2016) 3
- Bioorg Med Chem 18: 1149-62 (2010) 3
- J Med Chem 52: 4496-510 (2009) 3
- Bioorg Med Chem Lett 20: 453-7 (2010) 3
- ACS Med Chem Lett 3: 397-401 (2012) 3
- Bioorg Med Chem Lett 19: 639-43 (2009) 3
- Bioorg Med Chem Lett 21: 4913-8 (2011) 3
- Eur J Med Chem 62: 256-69 (2013) 2
- Bioorg Med Chem Lett 24: 4209-14 (2014) 2
- J Med Chem 55: 2820-34 (2012) 2
- Bioorg Med Chem Lett 20: 1278-83 (2010) 2
- Eur J Med Chem 43: 2627-38 (2008) 2
- Bioorg Med Chem Lett 18: 1199-206 (2008) 2
- Bioorg Med Chem 16: 7510-5 (2008) 2
- J Med Chem 48: 7486-90 (2005) 2
- J Med Chem 53: 1338-46 (2010) 2
- J Med Chem 47: 627-43 (2004) 2
- J Med Chem 62: 9806-9823 (2019) 2
- J Med Chem 52: 234-7 (2009) 2
- Bioorg Med Chem Lett 19: 6209-12 (2009) 2
- Bioorg Med Chem Lett 19: 2546-50 (2009) 2
- J Med Chem 58: 5751-69 (2015) 2
- J Med Chem 60: 1126-1141 (2017) 2
- J Med Chem 43: 2300-9 (2000) 2
- ...
Institutions 34▿
- Research Triangle Institute 14
- Green Cross 13
- North Carolina Central University 9
- Universit£ 7
- National Health Research Institutes 6
- Neuroscienze Pharmaness S.C.A R.L. 6
- National Institute Of Mental Health 6
- Rti International 6
- Vernalis (R&D) 5
- National Institute On Alcohol Abuse And Alcoholism 5
- Zhejiang University 5
- Forbes Norris Als/Mda Research Center 4
- Janssen Research & Development 4
- Amgen 4
- Cns Biological Research 4
- Neurogen 4
- Chinese Academy Of Sciences 4
- Solvay Pharma 4
- National Central University 4
- Instituto De Qu£Mica M£Dica 4
- TBA 3
- 7Tm Pharma 3
- Central Research Institute 3
- Dr. Reddy'S Laboratories 3
- University Of North Carolina At Greensboro 3
- University Of California 3
- University Of Bonn 3
- Msd 3
- Merck Research Laboratories 2
- Zydus Research Centre 2
- Julius-Maximilians-Universit£T W£Rzburg 2
- Università 2
- Pfizer 2
- University Of Salerno 2
- ...
Affinity: 0.11 to 1.3E+5 nM▿
- Ki 155
- IC50 79
- Kd 10
- EC50 24
- Affinity ≤ nM
Xtal structures: 0
Docked structures: 0
Catalog Cmpds: 1