BindingDB PrimarySearch

BDBM20557 AMG 517::CHEMBL229430::JMC503515 Compound 23::N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}oxy)-1,3-benzothiazol-2-yl]acetamide::US8796328, A::US8802711, H

SMILES: CC(=O)Nc1nc2c(Oc3cc(ncn3)-c3ccc(cc3)C(F)(F)F)cccc2s1

InChI Key: InChIKey=YUTIXVXZQIQWGY-UHFFFAOYSA-N

Data: 20 IC50

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 20 hits for monomerid = 20557
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
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	n/a	n/a
Amgen					Assay Description TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...				J Med Chem 50: 3515-27 (2007) Article DOI: 10.1021/jm070190p BindingDB Entry DOI: 10.7270/Q2RN364D
Amgen					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	n/a	n/a
Neurogen Corporation Curated by ChEMBL					Assay Description Inhibition of human TRPV1				J Med Chem 53: 3330-48 (2010) Article DOI: 10.1021/jm100051g BindingDB Entry DOI: 10.7270/Q2474BTP
Neurogen Corporation Curated by ChEMBL					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.620	n/a	n/a	n/a	n/a	n/a	n/a
Amgen					Assay Description TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...				J Med Chem 50: 3515-27 (2007) Article DOI: 10.1021/jm070190p BindingDB Entry DOI: 10.7270/Q2RN364D
Amgen					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.760	n/a	n/a	n/a	n/a	n/a	n/a
Amgen					Assay Description TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...				J Med Chem 50: 3515-27 (2007) Article DOI: 10.1021/jm070190p BindingDB Entry DOI: 10.7270/Q2RN364D
Amgen					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	7.4	22
Amgen					Assay Description TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...				J Med Chem 50: 3528-39 (2007) Article DOI: 10.1021/jm070191h BindingDB Entry DOI: 10.7270/Q2MW2FF4
Amgen					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.5	n/a	n/a	n/a	n/a	n/a	n/a
Amgen					Assay Description TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...				J Med Chem 50: 3528-39 (2007) Article DOI: 10.1021/jm070191h BindingDB Entry DOI: 10.7270/Q2MW2FF4
Amgen					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	US Patent	n/a	n/a	20	n/a	n/a	n/a	n/a	n/a	n/a
TBA US Patent					Assay Description The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2]i) using the Fluorescence...				US Patent US8796328 (2014) BindingDB Entry DOI: 10.7270/Q2639NFM
TBA US Patent					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	US Patent	n/a	n/a	20	n/a	n/a	n/a	n/a	n/a	n/a
AbbVie Inc. US Patent					Assay Description The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2+]i) using the Fluorescenc...				US Patent US8802711 (2014) BindingDB Entry DOI: 10.7270/Q2QZ28NC
AbbVie Inc. US Patent					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	US Patent	n/a	n/a	20	n/a	n/a	n/a	n/a	n/a	n/a
AbbVie Inc. US Patent					Assay Description The cDNA for human TRPV1 (hTRPV1) was isolated by reverse transcriptase-polymerase chain reaction (RT-PCR) from human small intestine poly A+ RNA sup...				US Patent US8969325 (2015) BindingDB Entry DOI: 10.7270/Q29P30BX
AbbVie Inc. US Patent					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.5	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of acid induced calcium influx				Bioorg Med Chem Lett 17: 6539-45 (2007) Article DOI: 10.1016/j.bmcl.2007.09.080 BindingDB Entry DOI: 10.7270/Q2FX7961
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.600	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Antagonist activity at human TRPV1 assessed as inhibition of low pH-induced calcium influx				J Med Chem 51: 2744-57 (2008) Article DOI: 10.1021/jm7014638 BindingDB Entry DOI: 10.7270/Q2930SZH
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.800	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced calcium influx				J Med Chem 51: 2744-57 (2008) Article DOI: 10.1021/jm7014638 BindingDB Entry DOI: 10.7270/Q2930SZH
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.5	n/a	n/a	n/a	n/a	5.0	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx				J Med Chem 51: 2744-57 (2008) Article DOI: 10.1021/jm7014638 BindingDB Entry DOI: 10.7270/Q2930SZH
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of capsaicin induced calcium influx				Bioorg Med Chem Lett 17: 6539-45 (2007) Article DOI: 10.1016/j.bmcl.2007.09.080 BindingDB Entry DOI: 10.7270/Q2FX7961
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx				J Med Chem 51: 2744-57 (2008) Article DOI: 10.1021/jm7014638 BindingDB Entry DOI: 10.7270/Q2930SZH
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced 45Ca2+ influx by FLIPR assay				Bioorg Med Chem Lett 18: 5118-22 (2008) Article DOI: 10.1016/j.bmcl.2008.07.112 BindingDB Entry DOI: 10.7270/Q27D2TXQ
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.5	n/a	n/a	n/a	n/a	5.0	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced 45Ca2+ influx by FLIPR assay				Bioorg Med Chem Lett 18: 5118-22 (2008) Article DOI: 10.1016/j.bmcl.2008.07.112 BindingDB Entry DOI: 10.7270/Q27D2TXQ
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Transient receptor potential cation channel subfamily V member 1 (Homo sapiens (Human))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.760	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization				Bioorg Med Chem Lett 18: 1830-4 (2008) Article DOI: 10.1016/j.bmcl.2008.02.022 BindingDB Entry DOI: 10.7270/Q2FB53SJ
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.900	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization				Bioorg Med Chem Lett 18: 1830-4 (2008) Article DOI: 10.1016/j.bmcl.2008.02.022 BindingDB Entry DOI: 10.7270/Q2FB53SJ
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Vanilloid receptor (Rattus norvegicus (rat))	BDBM20557 (AMG 517 \| CHEMBL229430 \| JMC503515 Compound 23 \| N...) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars	Article PubMed	n/a	n/a	0.5	n/a	n/a	n/a	n/a	n/a	n/a
Amgen					Assay Description TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...				J Med Chem 50: 3515-27 (2007) Article DOI: 10.1021/jm070190p BindingDB Entry DOI: 10.7270/Q2RN364D
Amgen					More data for this Ligand-Target Pair