BindingDB logo
myBDB logout

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

Find this compound or compounds like it in BindingDB or PDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 4 hits for monomerid = 426135   
Target/Host
(Institution)
LigandTarget/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
pHTemp
°C
Glutamate receptor AMPA 1/2


(Homo sapiens (Human))
BDBM426135
PNG
(5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...)
Show SMILES FC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H21F2N5O/c26-18-4-1-15(2-5-18)22-23(16-3-6-20-17(13-16)14-21(33)29-20)32-12-9-28-24(25(32)30-22)31-10-7-19(27)8-11-31/h1-6,9,12-13,19H,7-8,10-11,14H2,(H,29,33)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
US Patent
n/an/a 0.0800n/an/an/an/an/an/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
PNG
(5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...)
Show SMILES FC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H21F2N5O/c26-18-4-1-15(2-5-18)22-23(16-3-6-20-17(13-16)14-21(33)29-20)32-12-9-28-24(25(32)30-22)31-10-7-19(27)8-11-31/h1-6,9,12-13,19H,7-8,10-11,14H2,(H,29,33)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a 0.100n/an/an/an/an/an/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
PNG
(5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...)
Show SMILES FC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H21F2N5O/c26-18-4-1-15(2-5-18)22-23(16-3-6-20-17(13-16)14-21(33)29-20)32-12-9-28-24(25(32)30-22)31-10-7-19(27)8-11-31/h1-6,9,12-13,19H,7-8,10-11,14H2,(H,29,33)
PDB
MMDB

NCI pathway
Reactome pathway
KEGG

UniProtKB/SwissProt

B.MOAD
DrugBank
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a<1.00E+4n/an/an/an/an/an/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
PNG
(5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imid...)
Show SMILES FC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H21F2N5O/c26-18-4-1-15(2-5-18)22-23(16-3-6-20-17(13-16)14-21(33)29-20)32-12-9-28-24(25(32)30-22)31-10-7-19(27)8-11-31/h1-6,9,12-13,19H,7-8,10-11,14H2,(H,29,33)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a 100n/an/an/an/an/an/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