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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 270 hits for monomerid = 21278
Affinity DataEC50: 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
Affinity DataEC50: 0.170nMAssay Description:Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 0.310nMAssay Description:Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS bindingMore data for this Ligand-Target Pair
Affinity DataKi: 0.400nMAssay Description:Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.430nMAssay Description:Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS bindingMore data for this Ligand-Target Pair
Affinity DataKi: 0.650nM ΔG°: -12.7kcal/molepH: 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
Affinity DataKi: 0.700nMAssay Description:Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrometryMore data for this Ligand-Target Pair
Affinity DataKi: 0.730nMAssay Description:Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 0.740nMAssay Description:Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 0.900nM ΔG°: -12.5kcal/molepH: 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
Affinity DataKi: 0.900nMAssay Description:Displacement of [3H]SR141716A from rat brain CB1 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 0.933nMAssay Description:Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
Affinity DataKi: 1nMAssay Description:Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.10nMAssay Description:Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 1.10nMAssay Description:Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293T cell membranes by scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 1.18nMAssay Description:Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 1.18nMAssay Description:Binding affinity in a competition assay by displacement of [3H]- SR-141716 from Cannabinoid receptor 1 in rat whole brain membrane preparationMore data for this Ligand-Target Pair
Affinity DataKi: 1.18nMAssay Description:Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 1.23nMAssay Description:Displacement of [3H]SR141716A from CB1 receptor in rat cerebellumMore data for this Ligand-Target Pair
Affinity DataKi: 1.30nMAssay Description:Inhibition of [3H]CP-55940 binding to cannabinoid receptor 1 in rat brain membranes.More data for this Ligand-Target Pair
Affinity DataIC50: 1.35nMAssay Description:Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS levelMore data for this Ligand-Target Pair
Affinity DataKi: 1.40nMAssay Description:Displacement of [3H]CP-55940 from CB1 receptor by scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 1.40nMAssay Description:Displacement of [3H]CP55940 from CB1 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 1.5nMAssay Description:Displacement of [3H]CP55940 from CB1 receptor in CD1 mouse brain membrane without cerebellum by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: 1.60nMAssay Description:Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 1...More data for this Ligand-Target Pair
Affinity DataKi: 1.60nMAssay Description:Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 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
Affinity DataKi: 1.80nMAssay Description:Displacement of [3H]-CP55,940 from CB1 receptor in CD1 mouse brain membranes after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
Affinity DataKi: 1.80nMAssay Description:Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta countingMore data for this Ligand-Target Pair
Affinity DataKi: 1.80nMAssay Description:Displacement of [3H]CP-55940 from CB1 receptor in CD1 mouse brainMore data for this Ligand-Target Pair
Affinity DataKi: 1.80nMAssay Description:Binding affinity was determined by using a competition assay with [125 I]- AM251 against rat cannabinoid receptor 1More data for this Ligand-Target Pair
Affinity DataKd: 1.80nMAssay Description:Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 1.90nMAssay Description:Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation countingMore data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebella membraneMore data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetGTP-binding nuclear protein GSP1/CNR1(Baker's yeast)
Cns Biological Research
Curated by PDSP Ki Database
Cns Biological Research
Curated by PDSP Ki Database
Affinity DataKi: 1.98nMAssay Description:Displacement of [3H]WIN-55212-2 from CB1 receptor in rat cerebellar membrane by liquid scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 2nMAssay Description:Antagonist activity at CB1 receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 2nM ΔG°: -11.7kcal/molepH: 7.2 T: 2°CAssay Description:IC50 values for test compounds were determined from nonlinear regression analysis of data collected from ligand displacement experiments. The inhibit...More data for this Ligand-Target Pair
Affinity DataKi: 2.10nMAssay Description:Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 2.10nMAssay Description:Agonist activity at human CB1 receptor assessed as stimulation of [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
Affinity DataKd: 2.10nMpH: 7.4Assay Description:Briefly, ~5μg of membranes were incubated at 30 °C for 60 min with [3H]CP55940 (147.9 Ci/mmol; PerkinElmer Life Sciences) or [3H]SR141716A (43 C...More data for this Ligand-Target Pair
Affinity DataIC50: 2.20nMAssay Description:Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataKd: 2.40nMpH: 7.4Assay Description:Briefly, ~5μg of membranes were incubated at 30 °C for 60 min with [3H]CP55940 (147.9 Ci/mmol; PerkinElmer Life Sciences) or [3H]SR141716A (43 C...More data for this Ligand-Target Pair
Affinity DataKd: 2.40nMpH: 7.4Assay Description:Briefly, ~5μg of membranes were incubated at 30 °C for 60 min with [3H]CP55940 (147.9 Ci/mmol; PerkinElmer Life Sciences) or [3H]SR141716A (43 C...More data for this Ligand-Target Pair
Affinity DataKi: 2.40nMAssay Description:Binding affinity to human CB1 receptorMore data for this Ligand-Target Pair
Affinity DataKd: 2.5nMpH: 7.4Assay Description:Briefly, ~5μg of membranes were incubated at 30 °C for 60 min with [3H]CP55940 (147.9 Ci/mmol; PerkinElmer Life Sciences) or [3H]SR141716A (43 C...More data for this Ligand-Target Pair
Affinity DataKd: 2.5nMpH: 7.4Assay Description:Briefly, ~5μg of membranes were incubated at 30 °C for 60 min with [3H]CP55940 (147.9 Ci/mmol; PerkinElmer Life Sciences) or [3H]SR141716A (43 C...More data for this Ligand-Target Pair
