Compile Data Set for Download or QSAR
Report error Found 778 Enz. Inhib. hit(s) with Target = 'Glutamate receptor 1'
TargetGlutamate receptor 1(Rat)
University of Copenhagen

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50166288BDBM50166288((S)-2-Amino-3-[3-hydroxy-5-(2-methyl-2H-tetrazol-5...)
Affinity DataKi:  0.00520nMAssay Description:Displacement of [3H]AMPA from rat recombinant GluR1 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlutamate receptor 1(Rat)
University of Copenhagen

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50002370BDBM50002370((RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-p...)
Affinity DataKi:  0.0220nMAssay Description:Displacement of [3H]AMPA from rat recombinant GluR1 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426302BDBM426302(US10513523, Example 242 | 6-(7-Morpholino-2-phenyl...)
Affinity DataIC50: 0.0500nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426273BDBM426273(US10513523, Example 213 | 6-[7-(4-Methoxy-1-piperi...)
Affinity DataIC50: 0.0600nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426170BDBM426170(US10513523, Example 109 | 5-(2-(4-Fluorophenyl)-8-...)
Affinity DataIC50: 0.0600nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426136BDBM426136(US10513523, Example 75 | 5-[8-(4-Fluoro-1-piperidy...)
Affinity DataIC50: 0.0600nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426272BDBM426272(US10513523, Example 212 | 4-[3-(1H-Indazol-5-yl)-4...)
Affinity DataIC50: 0.0800nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426234BDBM426234(US10513523, Example 174 | 5-[2-(4-Fluorophenyl)-7-...)
Affinity DataIC50: 0.0800nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426135BDBM426135(US10513523, Example 74 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.0800nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426129BDBM426129(US10513523, Example 68 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.100nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 426135BDBM426135(US10513523, Example 74 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.100nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 426135BDBM426135(US10513523, Example 74 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.100nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426133BDBM426133(US10513523, Example 72 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.130nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426223BDBM426223(US10513523, Example 163 | 5-[5-Chloro-2-(4-fluorop...)
Affinity DataIC50: 0.130nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426268BDBM426268(US10513523, Example 208 | 5-(4-Methyl-7-morpholino...)
Affinity DataIC50: 0.130nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Rat)
University of Copenhagen

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50166286BDBM50166286((RS)-2-amino-3-[3-hydroxy-5-(2-ethyl-2H-5-tetrazol...)
Affinity DataKi:  0.150nMAssay Description:Displacement of [3H]AMPA from rat recombinant GluR1 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426131BDBM426131(US10513523, Example 70 | (trans)-5-[8-(3-Fluoro-4-...)
Affinity DataIC50: 0.160nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426245BDBM426245(US10513523, Example 185 | 5-(2-(4-Fluorophenyl)-8-...)
Affinity DataIC50: 0.160nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426126BDBM426126(US10513523, Example 65 | 5-(8-Morpholino-2-phenyl-...)
Affinity DataIC50: 0.160nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426247BDBM426247(US10513523, Example 187 | 5-[7-(4-Hydroxy-1-piperi...)
Affinity DataIC50: 0.160nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426249BDBM426249(US10513523, Example 189 | 5-[7-(4-Methoxy-1-piperi...)
Affinity DataIC50: 0.160nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426232BDBM426232(US10513523, Example 172 | 5-[7-(4-Acetylpiperazin-...)
Affinity DataIC50: 0.160nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-8 subunit(Human)
Janssen Research & Development

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50459036BDBM50459036(CHEMBL4211865)
Affinity DataIC50: 0.200nMAssay Description:Modulation of recombinant human GluA1 flop isoform/TARPgamma8 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 426226BDBM426226(US10513523, Example 166 | 5-[2-(4-Fluorophenyl)-7-...)
Affinity DataIC50: 0.200nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426226BDBM426226(US10513523, Example 166 | 5-[2-(4-Fluorophenyl)-7-...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426116BDBM426116(US10513523, Example 55 | 5-[8-(1,4-Dioxa-8-azaspir...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426094BDBM426094(US10513523, Example 33 | 4-[2-(4-Fluorophenyl)-3-(...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426074BDBM426074(1-[4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidaz...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426250BDBM426250(US10513523, Example 190 | 5-[2-(4-Fluorophenyl)-7-...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426237BDBM426237(US10513523, Example 177 | 5-[2-(4-Fluorophenyl)-7-...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426069BDBM426069(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426246BDBM426246(US10513523, Example 186 | 5-[2-(4-Fluorophenyl)-7-...)
Affinity DataIC50: 0.200nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426132BDBM426132(US10513523, Example 71 | 5-[8-(3,3-Difluoro-4-hydr...)
Affinity DataIC50: 0.25nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426137BDBM426137(US10513523, Example 76 | 5-[8-[4-(Fluoromethyl)-1-...)
Affinity DataIC50: 0.25nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 426232BDBM426232(US10513523, Example 172 | 5-[7-(4-Acetylpiperazin-...)
Affinity DataIC50: 0.251nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426115BDBM426115(US10513523, Example 54 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426098BDBM426098(US10513523, Example 37 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426178BDBM426178(US10513523, Example 118 | 6-[2-(4-Fluorophenyl)-8-...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426213BDBM426213(US10513523, Example 153 | 5-(2-Benzoyl-8-morpholin...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426143BDBM426143(US10513523, Example 82 | 5-[5-Chloro-2-(4-fluoroph...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426174BDBM426174(US10513523, Example 113 | 5-(8-(4-Acetylpiperazin-...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426097BDBM426097(US10513523, Example 36 | tert-Butyl 4-[2-benzyl-3-...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426253BDBM426253(US10513523, Example 193 | trans-5-[7-(3-Fluoro-4-h...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426134BDBM426134(US10513523, Example 73 | (cis)-5-[8-(3-Fluoro-4-hy...)
Affinity DataIC50: 0.320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 426098BDBM426098(US10513523, Example 37 | 5-[2-(4-Fluorophenyl)-8-(...)
Affinity DataIC50: 0.398nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetGlutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit(Human)
Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 426073BDBM426073(5-[8-(4-Acetylpiperazin-1-yl)-2-(4-fluorophenyl)im...)
Affinity DataIC50: 0.398nMAssay Description:Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293 cells assessed as inhibition of glutamate-induc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426293BDBM426293(US10513523, Example 233 | 4-[3-(1H-Indazol-5-yl)-2...)
Affinity DataIC50: 0.400nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426142BDBM426142(US10513523, Example 81 | 5-[8-(3-Fluoroazetidin-1-...)
Affinity DataIC50: 0.400nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426267BDBM426267(US10513523, Example 207 | 5-(4-Bromo-7-morpholino-...)
Affinity DataIC50: 0.400nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

TargetGlutamate receptor 1(Human)
Janssen Pharmaceutica

US Patent
LigandChemical structure of BindingDB Monomer ID 426138BDBM426138(US10513523, Example 77 | 5-[8-[4-(2-Fluoroethyl)-1...)
Affinity DataIC50: 0.400nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/24/2020
Entry Details
US Patent

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