BindingDB PrimarySearch

BDBM154245 US9012443, 261

SMILES: COc1cc(ccc1-c1ncnc2cc(ccc12)S(=O)(=O)Nc1nccs1)C(F)(F)F

InChI Key: InChIKey=VSUDRCZPHWUXEW-UHFFFAOYSA-N

Data: 22 IC50

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 22 hits for monomerid = 154245
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
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	US Patent	n/a	n/a	10	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. US Patent					Assay Description 293 Cells stably transfected with either Nav 1.7 or Nav 1.5 were recorded in population patch-clamp mode with the IonWorks Quattro automated electrop...				US Patent US9012443 (2015) BindingDB Entry DOI: 10.7270/Q2N0158J
Amgen Inc. US Patent					More data for this Ligand-Target Pair
Cytochrome P450 3A4 (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	>5.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Inhibition of CYP3A4 (unknown origin)				J Med Chem 60: 5969-5989 (2017) Article DOI: 10.1021/acs.jmedchem.6b01851 BindingDB Entry DOI: 10.7270/Q2RJ4MS7
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 5 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	US Patent	n/a	n/a	>3.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. US Patent					Assay Description 293 cells stably transfected with Nav 1.5 were recorded in whole cell voltage clamp mode with the PatchXpress automated electrophysiology system acco...				US Patent US9012443 (2015) BindingDB Entry DOI: 10.7270/Q2N0158J
Amgen Inc. US Patent					More data for this Ligand-Target Pair
Sodium channel protein type 8 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	3.70E+3	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.6 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type IX alpha subunit (Rattus norvegicus)	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB MMDB KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	3.50E+3	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated rat Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell v...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 5 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	>3.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of human Nav1.5 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 min...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	9	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -60 mV measured for 3 to 5 mins...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Mus musculus)	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	180	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated mouse Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell ...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel alpha subunit (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	7.30E+3	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.1 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.3 (Nav1.3) (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	2.10E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.3 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 5 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	1.60E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.5 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 10 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	>3.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.8 expressed in CHO cells assessed as inhibition of TTX-resistant current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
1,3-beta-glucan synthase component GLS2 (Saccharomyces cerevisiae)	BDBM154245 (US9012443, 261) Show SMILES Show InChI	KEGG UniProtKB/SwissProt GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	>3.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes measured after 90 mins by TopCount scintillation counting method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Mus musculus)	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	130	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated Nav1.7 in C57BL/6 mouse DRG neurons assessed as inhibition of sodium currents in presence of TTX by whole cell patch cl...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	160	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 min...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	7.20E+3	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of human Nav1.7 in closed state expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -140 mV measure...				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 2 alpha subunit (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	2.10E+3	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.2 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	140	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.7 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.4 (Nav1.4) (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	1.70E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen, Inc. Curated by ChEMBL					Assay Description Inhibition of 20% inactivated human Nav1.4 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method				ACS Med Chem Lett 7: 1062-1067 (2016) Article DOI: 10.1021/acsmedchemlett.6b00243 BindingDB Entry DOI: 10.7270/Q2VM4F65
Amgen, Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	160	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assay				J Med Chem 60: 5969-5989 (2017) Article DOI: 10.1021/acs.jmedchem.6b01851 BindingDB Entry DOI: 10.7270/Q2RJ4MS7
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 5 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	Article PubMed	n/a	n/a	>3.00E+4	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. Curated by ChEMBL					Assay Description Inhibition of human Nav1.5 expressed in HEK293 cells assessed as reduction in peak inward current by ionworks quattro electrophysiology assay				J Med Chem 60: 5969-5989 (2017) Article DOI: 10.1021/acs.jmedchem.6b01851 BindingDB Entry DOI: 10.7270/Q2RJ4MS7
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human))	BDBM154245 (US9012443, 261) Show SMILES Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase MCE PC cid PC sid UniChem Similars	US Patent	n/a	n/a	200	n/a	n/a	n/a	n/a	n/a	n/a
Amgen Inc. US Patent					Assay Description 293 cells stably transfected with human Nav1.7 were recorded in whole cell voltage clamp mode with the PatchXpress automated electrophysiology system...				US Patent US9012443 (2015) BindingDB Entry DOI: 10.7270/Q2N0158J
Amgen Inc. US Patent					More data for this Ligand-Target Pair