BDBM371590 (R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluoromethyl)phenyl)-N-(pyrimidin-2-yl) chromane-7-sulfonamide::US10239869, Example 16
SMILES: Cn1nccc1-c1cc(ccc1[C@H]1CCOc2cc(ccc12)S(=O)(=O)Nc1ncccn1)C(F)(F)F
InChI Key: InChIKey=LARCZEQUTRFGKA-GOSISDBHSA-N
Data: 8 IC50
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 17 | n/a | n/a | n/a | n/a | n/a | n/a |
University of California at San Francisco | Assay Description HEK-293 cells overexpressing the channel of interest were seeded in a 96-well plate at a density of 30000 cells/well and incubated at 37° C./5% CO2 f... | J Med Chem 51: 545-52 (2008) BindingDB Entry DOI: 10.7270/Q2NG4SZX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 5 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of California at San Francisco | Assay Description HEK-293 cells overexpressing the channel of interest were seeded in a 96-well plate at a density of 30000 cells/well and incubated at 37° C./5% CO2 f... | J Med Chem 51: 545-52 (2008) BindingDB Entry DOI: 10.7270/Q2NG4SZX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | PubMed | n/a | n/a | 9.50E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Lupin Ltd. Curated by ChEMBL | Assay Description Inhibition of human Nav1.7 at resting state expressed in HEK293 cells at -120 mV holding potential by 10 Hz single pulse protocol based manual patch ... | J Med Chem 63: 6107-6133 (2020) | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | PubMed | n/a | n/a | 30 | n/a | n/a | n/a | n/a | n/a | n/a |
Lupin Ltd. Curated by ChEMBL | Assay Description Use-dependent inhibition of human Nav1.7 expressed in HEK293 cells at 25 pulse 10 Hz frequency at -120 mV holding potential by manual patch clamp ass... | J Med Chem 63: 6107-6133 (2020) | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | PubMed | n/a | n/a | 18 | n/a | n/a | n/a | n/a | n/a | n/a |
Lupin Ltd. Curated by ChEMBL | Assay Description Inhibition of Nav1.7 (unknown origin) expressed in HEK293 cells assessed as reduction in veratridine-induced depolarization preincubated for 15 to 20... | J Med Chem 63: 6107-6133 (2020) | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | PubMed | n/a | n/a | 16 | n/a | n/a | n/a | n/a | n/a | n/a |
Lupin Ltd. Curated by ChEMBL | Assay Description Inhibition of human Nav1.7 expressed in HEK293 cells assessed as V1/2 of slow inactivation at 10 Hz frequency at -120 mV holding potential by single ... | J Med Chem 63: 6107-6133 (2020) | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 9 subunit alpha (Homo sapiens (Human)) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | PubMed | n/a | n/a | 45 | n/a | n/a | n/a | n/a | n/a | n/a |
Lupin Ltd. Curated by ChEMBL | Assay Description Inhibition of human Nav1.7 expressed in HEK293 cells assessed as V1/2 of fast inactivation at 10 Hz frequency at -120 mV holding potential by single ... | J Med Chem 63: 6107-6133 (2020) | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Sodium channel protein type 9 subunit alpha (Mus musculus) | BDBM371590 ((R)-4-(2-(1-Methyl-1H-pyrazol-5-yl)-4-(trifluorome...) | PDB UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet | PC cid PC sid UniChem | PubMed | n/a | n/a | 33 | n/a | n/a | n/a | n/a | n/a | n/a |
Lupin Ltd. Curated by ChEMBL | Assay Description Inhibition of mouse Nav1.7 expressed in HEK293 cells assessed as reduction in veratridine-induced depolarization preincubated for 15 to 20 mins follo... | J Med Chem 63: 6107-6133 (2020) | |||||||||||
More data for this Ligand-Target Pair |