BDBM426135 5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imidazo[1,2-a]pyrazin-3-::US10513523, Example 74
SMILES: FC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
InChI Key: InChIKey=CQHVKBXXQZUVDK-UHFFFAOYSA-N
Data: 4 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 |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Glutamate receptor AMPA 1/2 (Homo sapiens (Human)) | BDBM426135 (5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 0.0800 | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Pharmaceutica NV US Patent | Assay Description This assay was used to test compounds for their ability to inhibit TARP γ8 dependent AMPA receptor activity. The AMPA receptor is a non-selectiv... | US Patent US10513523 (2019) BindingDB Entry DOI: 10.7270/Q2KW5JDR | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
GRIA1/CACNG2 (Homo sapiens (Human)) | BDBM426135 (5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | Article PubMed | n/a | n/a | 0.100 | n/a | n/a | n/a | n/a | n/a | n/a |
Sanford Burnham Prebys Medical Discovery Institute Curated by ChEMBL | Assay Description Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc... | ACS Med Chem Lett 10: 267-272 (2019) Article DOI: 10.1021/acsmedchemlett.8b00599 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Voltage-dependent calcium channel gamma-8 subunit (Rattus norvegicus) | BDBM426135 (5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...) | PDB MMDB NCI pathway Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank GoogleScholar AffyNet | PC cid PC sid UniChem | Article PubMed | n/a | n/a | <1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Sanford Burnham Prebys Medical Discovery Institute Curated by ChEMBL | Assay Description Negative allosteric modulation of TARPgamma8 in rat hippocampal neurons assessed as inhibition of glutamate-induced current at 10 uM at -60 mV holdin... | ACS Med Chem Lett 10: 267-272 (2019) Article DOI: 10.1021/acsmedchemlett.8b00599 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
GRIA1/CACNG2 (Homo sapiens (Human)) | BDBM426135 (5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | Article PubMed | n/a | n/a | 100 | n/a | n/a | n/a | n/a | n/a | n/a |
Sanford Burnham Prebys Medical Discovery Institute Curated by ChEMBL | Assay Description Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc... | ACS Med Chem Lett 10: 267-272 (2019) Article DOI: 10.1021/acsmedchemlett.8b00599 | |||||||||||
More data for this Ligand-Target Pair |