BindingDB PrimarySearch

BDBM21279 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide::AM 251::AM-251::AM251::CHEMBL285932::N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide

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

InChI Key: InChIKey=BUZAJRPLUGXRAB-UHFFFAOYSA-N

Data: 18 KI 2 IC50 3 EC50

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 23 hits for monomerid = 21279
Target/Host (Institution)	Ligand	Target/Host Links	Ligand Links	Trg + Lig Links	Ki nM	ΔG° kcal/mole	IC50 nM	Kd nM	EC50/IC50 nM	k_off s^-1	k_on M^-1s^-1	pH	Temp °C
Cannabinoid receptor 1 (Rattus norvegicus (rat))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	0.600	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
National Institute on Drug Abuse Curated by ChEMBL					Assay Description Binding affinity was determined by using a competition assay with [125 I]- AM251 against rat cannabinoid receptor 1				J Med Chem 46: 642-5 (2003) Article DOI: 10.1021/jm020157x BindingDB Entry DOI: 10.7270/Q27M079X
National Institute on Drug Abuse Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	2.30	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Sapienza Universit�adi Roma					Assay Description IC50 values for test compounds were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibition c...				J Med Chem 51: 1560-76 (2008) Article DOI: 10.1021/jm070566z BindingDB Entry DOI: 10.7270/Q2GX48V9
Sapienza Universit�adi Roma					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	2.30	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
University of Salerno Curated by ChEMBL					Assay Description Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells				Bioorg Med Chem 16: 7510-5 (2008) Article DOI: 10.1016/j.bmc.2008.06.001 BindingDB Entry DOI: 10.7270/Q2C53MSN
University of Salerno Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	2.30	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Sapienza Universit£ di Roma Curated by ChEMBL					Assay Description Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells				Bioorg Med Chem 17: 5549-64 (2009) Article DOI: 10.1016/j.bmc.2009.06.027 BindingDB Entry DOI: 10.7270/Q2XK8GHD
Sapienza Universit£ di Roma Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	2.30	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Sapienza Universit£ di Roma Curated by ChEMBL					Assay Description Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells				Eur J Med Chem 45: 5878-86 (2010) Article DOI: 10.1016/j.ejmech.2010.09.053 BindingDB Entry DOI: 10.7270/Q22Z15T3
Sapienza Universit£ di Roma Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	3	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Pharmaceutical Research Institute Curated by ChEMBL					Assay Description Binding affinity to human CB1 receptor				Bioorg Med Chem Lett 17: 3978-82 (2007) Article DOI: 10.1016/j.bmcl.2007.04.087 BindingDB Entry DOI: 10.7270/Q2FN15XR
Pharmaceutical Research Institute Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Rattus norvegicus (rat))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	PubMed	6	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
University of South Carolina Curated by ChEMBL					Assay Description Inhibition of [3H]-CP-55,940 binding to cannabinoid receptor 1 in rat brain membranes.				J Med Chem 45: 1447-59 (2002) BindingDB Entry DOI: 10.7270/Q2222T3Z
University of South Carolina Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	7.49	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Binding affinity to cannabinoid CB1 receptor				J Med Chem 53: 4332-53 (2010) Article DOI: 10.1021/jm9018756 BindingDB Entry DOI: 10.7270/Q21R6QPF
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Rattus norvegicus (rat))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	7.49	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
University of Connecticut Curated by ChEMBL					Assay Description Binding affinity against Cannabinoid receptor 1 in rat forebrain				J Med Chem 42: 769-76 (1999) Article DOI: 10.1021/jm980363y BindingDB Entry DOI: 10.7270/Q2FJ2FZV
University of Connecticut Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article	7.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
TBA					Assay Description Antagonist activity at CB1 receptor (unknown origin)				Citation and Details Article DOI: 10.1007/s00044-012-0418-y BindingDB Entry DOI: 10.7270/Q2WS8X4M
TBA					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article	7.5	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
TBA					Assay Description Antagonist activity at CB1 receptor (unknown origin)				Citation and Details Article DOI: 10.1007/s00044-012-0418-y BindingDB Entry DOI: 10.7270/Q2WS8X4M
TBA					More data for this Ligand-Target Pair
Cannabinoid receptor (Rattus norvegicus (Rat)-Rattus norvegicus (rat))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	69	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Biological Research Centre of the Hungarian Academy of Sciences Curated by ChEMBL					Assay Description Displacement of [3H]JWH-018 from CB1R/CB2R in Wistar rat brain membranes after 60 mins by liquid scintillation analysis				Eur J Med Chem 178: 571-588 (2019) Article DOI: 10.1016/j.ejmech.2019.05.037
					More data for this Ligand-Target Pair
Cannabinoid receptor 2 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	110	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
University of Salerno Curated by ChEMBL					Assay Description Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells				Bioorg Med Chem 16: 7510-5 (2008) Article DOI: 10.1016/j.bmc.2008.06.001 BindingDB Entry DOI: 10.7270/Q2C53MSN
University of Salerno Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 2 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	112	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Sapienza Universit£ di Roma Curated by ChEMBL					Assay Description Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells				Eur J Med Chem 45: 5878-86 (2010) Article DOI: 10.1016/j.ejmech.2010.09.053 BindingDB Entry DOI: 10.7270/Q22Z15T3
Sapienza Universit£ di Roma Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 2 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	112	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Sapienza Universit£ di Roma Curated by ChEMBL					Assay Description Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells				Bioorg Med Chem 17: 5549-64 (2009) Article DOI: 10.1016/j.bmc.2009.06.027 BindingDB Entry DOI: 10.7270/Q2XK8GHD
Sapienza Universit£ di Roma Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 2 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	112	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Sapienza Universit�adi Roma					Assay Description IC50 values for test compounds were determined from nonlinear regression analysis of data collected from ligand binding experiments. The inhibition c...				J Med Chem 51: 1560-76 (2008) Article DOI: 10.1021/jm070566z BindingDB Entry DOI: 10.7270/Q2GX48V9
Sapienza Universit�adi Roma					More data for this Ligand-Target Pair
Cannabinoid receptor 2 (MOUSE)	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	2.29E+3	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
University of Connecticut Curated by ChEMBL					Assay Description Binding affinity against Cannabinoid receptor 2 in mouse spleen				J Med Chem 42: 769-76 (1999) Article DOI: 10.1021/jm980363y BindingDB Entry DOI: 10.7270/Q2FJ2FZV
University of Connecticut Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 2 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	2.29E+3	n/a	n/a	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Binding affinity to cannabinoid CB2 receptor				J Med Chem 53: 4332-53 (2010) Article DOI: 10.1021/jm9018756 BindingDB Entry DOI: 10.7270/Q21R6QPF
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	n/a	n/a	68	n/a	n/a	n/a	n/a
Julius-Maximilians-Universit£t W£rzburg Curated by ChEMBL					Assay Description Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP af...				Bioorg Med Chem Lett 24: 4209-14 (2014) Article DOI: 10.1016/j.bmcl.2014.07.038 BindingDB Entry DOI: 10.7270/Q26M38HV
Julius-Maximilians-Universit£t W£rzburg Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	n/a	n/a	58	n/a	n/a	n/a	n/a
Julius-Maximilians-Universit£t W£rzburg Curated by ChEMBL					Assay Description Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Galpha i2 assessed as Galpha GTPase activity using [gamma-33P]GTP ...				Bioorg Med Chem 22: 3938-46 (2014) Article DOI: 10.1016/j.bmc.2014.06.008 BindingDB Entry DOI: 10.7270/Q2862J3W
Julius-Maximilians-Universit£t W£rzburg Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	n/a	n/a	70	n/a	n/a	n/a	n/a
Julius-Maximilians-Universit£t W£rzburg Curated by ChEMBL					Assay Description Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP af...				Bioorg Med Chem Lett 24: 4209-14 (2014) Article DOI: 10.1016/j.bmcl.2014.07.038 BindingDB Entry DOI: 10.7270/Q26M38HV
Julius-Maximilians-Universit£t W£rzburg Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.320	n/a	n/a	n/a	n/a	n/a	n/a
Merck Research Laboratories Curated by ChEMBL					Assay Description Displacement of [3H]SR-141716 from human wild type CB1R expressed in CHO cells				J Med Chem 51: 2108-14 (2008) Article DOI: 10.1021/jm7014974 BindingDB Entry DOI: 10.7270/Q27H1KDR
Merck Research Laboratories Curated by ChEMBL					More data for this Ligand-Target Pair
Cannabinoid receptor 1 (Homo sapiens (Human))	BDBM21279 (1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N...) Show SMILES Show InChI	PDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	3.5	n/a	n/a	n/a	n/a	n/a	n/a
Merck Research Laboratories Curated by ChEMBL					Assay Description Displacement of [3H]CP-55940 from human wild type CB1R expressed in CHO cells				J Med Chem 51: 2108-14 (2008) Article DOI: 10.1021/jm7014974 BindingDB Entry DOI: 10.7270/Q27H1KDR
Merck Research Laboratories Curated by ChEMBL					More data for this Ligand-Target Pair