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Compile Data Set for Download or QSAR

Found 33 hits of ic50 for UniProtKB: P42261   
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 1/Voltage-dependent calcium channel gamma-2 subunit


(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)
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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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(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)
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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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426226
PNG
(5-[2-(4-Fluorophenyl)-7-(4-hydroxy-1-piperidyl)pyr...)
Show SMILES OC1CCN(CC1)c1nccc2c(c(nn12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H22FN5O2/c26-18-4-1-15(2-5-18)24-23(16-3-6-20-17(13-16)14-22(33)28-20)21-7-10-27-25(31(21)29-24)30-11-8-19(32)9-12-30/h1-7,10,13,19,32H,8-9,11-12,14H2,(H,28,33)
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n/an/a 0.200n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426232
PNG
(5-[7-(4-Acetylpiperazin-1-yl)-2-(4-fluorophenyl)py...)
Show SMILES CC(=O)N1CCN(CC1)c1nccc2c(c(nn12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C26H23FN6O2/c1-16(34)31-10-12-32(13-11-31)26-28-9-8-22-24(18-4-7-21-19(14-18)15-23(35)29-21)25(30-33(22)26)17-2-5-20(27)6-3-17/h2-9,14H,10-13,15H2,1H3,(H,29,35)
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n/an/a 0.251n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426073
PNG
(5-[8-(4-Acetylpiperazin-1-yl)-2-(4-fluorophenyl)im...)
Show SMILES CC(=O)N1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C26H23FN6O2/c1-16(34)31-10-12-32(13-11-31)25-26-30-23(17-2-5-20(27)6-3-17)24(33(26)9-8-28-25)18-4-7-21-19(14-18)15-22(35)29-21/h2-9,14H,10-13,15H2,1H3,(H,29,35)
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n/an/a 0.398n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426098
PNG
(5-[2-(4-Fluorophenyl)-8-(4-hydroxy-1-piperidyl)imi...)
Show SMILES OC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H22FN5O2/c26-18-4-1-15(2-5-18)22-23(16-3-6-20-17(13-16)14-21(33)28-20)31-12-9-27-24(25(31)29-22)30-10-7-19(32)8-11-30/h1-6,9,12-13,19,32H,7-8,10-11,14H2,(H,28,33)
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n/an/a 0.398n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426224
PNG
(5-[2-(4-Fluorophenyl)-7-morpholino-pyrazolo[1,5-c]...)
Show SMILES Fc1ccc(cc1)-c1nn2c(nccc2c1-c1ccc2NC(=O)Cc2c1)N1CCOCC1
Show InChI InChI=1S/C24H20FN5O2/c25-18-4-1-15(2-5-18)23-22(16-3-6-19-17(13-16)14-21(31)27-19)20-7-8-26-24(30(20)28-23)29-9-11-32-12-10-29/h1-8,13H,9-12,14H2,(H,27,31)
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n/an/a 0.501n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426093
PNG
(5-[2-(4-Fluorophenyl)-8-(3-oxopiperazin-1-yl)imida...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2NC(=O)Cc2c1)N1CCNC(=O)C1
Show InChI InChI=1S/C24H19FN6O2/c25-17-4-1-14(2-5-17)21-22(15-3-6-18-16(11-15)12-19(32)28-18)31-10-8-27-23(24(31)29-21)30-9-7-26-20(33)13-30/h1-6,8,10-11H,7,9,12-13H2,(H,26,33)(H,28,32)
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n/an/a 0.501n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426069
PNG
(5-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2NC(=O)Cc2c1)N1CCOCC1
Show InChI InChI=1S/C24H20FN5O2/c25-18-4-1-15(2-5-18)21-22(16-3-6-19-17(13-16)14-20(31)27-19)30-8-7-26-23(24(30)28-21)29-9-11-32-12-10-29/h1-8,13H,9-12,14H2,(H,27,31)
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n/an/a 0.501n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426071
PNG
(4-[2-(4-Fluorophenyl)-3-(1H-indazol-5-yl)imidazo[1...)
Show SMILES Fc1ccc(cc1)-c1nc2c(nccn2c1-c1ccc2[nH]ncc2c1)N1CCOCC1
Show InChI InChI=1S/C23H19FN6O/c24-18-4-1-15(2-5-18)20-21(16-3-6-19-17(13-16)14-26-28-19)30-8-7-25-22(23(30)27-20)29-9-11-31-12-10-29/h1-8,13-14H,9-12H2,(H,26,28)
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n/an/a 0.631n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426228
PNG
(5-[2-(4-Fluorophenyl)-7-(3-oxopiperazin-1-yl)pyraz...)
Show SMILES Fc1ccc(cc1)-c1nn2c(nccc2c1-c1ccc2NC(=O)Cc2c1)N1CCNC(=O)C1
Show InChI InChI=1S/C24H19FN6O2/c25-17-4-1-14(2-5-17)23-22(15-3-6-18-16(11-15)12-20(32)28-18)19-7-8-27-24(31(19)29-23)30-10-9-26-21(33)13-30/h1-8,11H,9-10,12-13H2,(H,26,33)(H,28,32)
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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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426250
PNG
(5-[2-(4-Fluorophenyl)-7-(4-fluoro-1-piperidyl)pyra...)
Show SMILES FC1CCN(CC1)c1nccc2c(c(nn12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C25H21F2N5O/c26-18-4-1-15(2-5-18)24-23(16-3-6-20-17(13-16)14-22(33)29-20)21-7-10-28-25(32(21)30-24)31-11-8-19(27)9-12-31/h1-7,10,13,19H,8-9,11-12,14H2,(H,29,33)
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n/an/a 5n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50509857
PNG
(CHEMBL4474333)
Show SMILES Oc1ccc(cc1)-c1c(nc2c(nccn12)N1CCOCC1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C22H19ClN4O2/c23-17-5-1-15(2-6-17)19-20(16-3-7-18(28)8-4-16)27-10-9-24-21(22(27)25-19)26-11-13-29-14-12-26/h1-10,28H,11-14H2
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n/an/a 10n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM426144
PNG
(4-[2-(4-Fluorophenyl)-8-morpholino-imidazo[1,2-a]p...)
Show SMILES Oc1ccc(cc1)-c1c(nc2c(nccn12)N1CCOCC1)-c1ccc(F)cc1
Show InChI InChI=1S/C22H19FN4O2/c23-17-5-1-15(2-6-17)19-20(16-3-7-18(28)8-4-16)27-10-9-24-21(22(27)25-19)26-11-13-29-14-12-26/h1-10,28H,11-14H2
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n/an/a 13n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50509856
PNG
(CHEMBL4533591)
Show SMILES Nc1ccc(cc1)-c1c(nc2c(nccn12)N1CCOCC1)-c1ccc(F)cc1
Show InChI InChI=1S/C22H20FN5O/c23-17-5-1-15(2-6-17)19-20(16-3-7-18(24)8-4-16)28-10-9-25-21(22(28)26-19)27-11-13-29-14-12-27/h1-10H,11-14,24H2
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n/an/a 63n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50509859
PNG
(CHEMBL4458004)
Show SMILES COc1ccc(cc1)-c1c(nc2c(nccn12)N1CCOCC1)-c1ccc(F)cc1
Show InChI InChI=1S/C23H21FN4O2/c1-29-19-8-4-17(5-9-19)21-20(16-2-6-18(24)7-3-16)26-23-22(25-10-11-28(21)23)27-12-14-30-15-13-27/h2-11H,12-15H2,1H3
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n/an/a 501n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50509858
PNG
(CHEMBL4526929)
Show SMILES Oc1ccc(cc1)-n1c(nc2ccccc12)-c1ccc(F)cc1
Show InChI InChI=1S/C19H13FN2O/c20-14-7-5-13(6-8-14)19-21-17-3-1-2-4-18(17)22(19)15-9-11-16(23)12-10-15/h1-12,23H
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n/an/a 1.26E+3n/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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459030
PNG
(CHEMBL4207238 | US10611730, Example 124)
Show SMILES Clc1cccc(CC#N)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C15H10ClN3O/c16-11-3-1-2-9(6-7-17)14(11)10-4-5-12-13(8-10)19-15(20)18-12/h1-5,8H,6H2,(H2,18,19,20)
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n/an/a<1.00E+4n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459029
PNG
(CHEMBL4218962 | US10611730, Example 56)
Show SMILES Clc1cccc(C#N)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C14H8ClN3O/c15-10-3-1-2-9(7-16)13(10)8-4-5-11-12(6-8)18-14(19)17-11/h1-6H,(H2,17,18,19)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459028
PNG
(CHEMBL4216045 | US10611730, Example 160)
Show SMILES Clc1cccc(C2CC2)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C16H13ClN2O/c17-12-3-1-2-11(9-4-5-9)15(12)10-6-7-13-14(8-10)19-16(20)18-13/h1-3,6-9H,4-5H2,(H2,18,19,20)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50509855
PNG
(CHEMBL4545322)
Show SMILES CC(=O)Nc1ccc(cc1)-c1c(nc2c(nccn12)N1CCOCC1)-c1ccc(F)cc1
Show InChI InChI=1S/C24H22FN5O2/c1-16(31)27-20-8-4-18(5-9-20)22-21(17-2-6-19(25)7-3-17)28-24-23(26-10-11-30(22)24)29-12-14-32-15-13-29/h2-11H,12-15H2,1H3,(H,27,31)
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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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50509854
PNG
(CHEMBL4439385)
Show SMILES COCCn1cc(cn1)-c1c(nc2c(nccn12)N1CCOCC1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C22H23ClN6O2/c1-30-11-10-28-15-17(14-25-28)20-19(16-2-4-18(23)5-3-16)26-22-21(24-6-7-29(20)22)27-8-12-31-13-9-27/h2-7,14-15H,8-13H2,1H3
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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
BindingDB Entry DOI: 10.7270/Q26H4MRG
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459027
PNG
(CHEMBL4214773)
Show SMILES Cc1ccccc1-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C15H13NO/c1-10-4-2-3-5-13(10)11-6-7-14-12(8-11)9-15(17)16-14/h2-8H,9H2,1H3,(H,16,17)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459026
PNG
(CHEMBL4214902 | US10611730, Example 31)
Show SMILES FC(F)(F)Oc1cccc(Cl)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C14H8ClF3N2O2/c15-8-2-1-3-11(22-14(16,17)18)12(8)7-4-5-9-10(6-7)20-13(21)19-9/h1-6H,(H2,19,20,21)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459023
PNG
(CHEMBL4202885 | US10611730, Example 69)
Show SMILES Clc1cncc(Cl)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C12H7Cl2N3O/c13-7-4-15-5-8(14)11(7)6-1-2-9-10(3-6)17-12(18)16-9/h1-5H,(H2,16,17,18)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459025
PNG
(CHEMBL4211593 | US10611730, Example 2)
Show SMILES Cc1cccc(C)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C15H14N2O/c1-9-4-3-5-10(2)14(9)11-6-7-12-13(8-11)17-15(18)16-12/h3-8H,1-2H3,(H2,16,17,18)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459022
PNG
(CHEMBL4214549 | US10611730, Example 49)
Show SMILES Clc1cccc(Cl)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C13H8Cl2N2O/c14-8-2-1-3-9(15)12(8)7-4-5-10-11(6-7)17-13(18)16-10/h1-6H,(H2,16,17,18)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459032
PNG
(CHEMBL4215352)
Show SMILES Cc1cc(cc2CC(=O)Nc12)-c1c(Cl)cncc1OC(F)F
Show InChI InChI=1S/C15H11ClF2N2O2/c1-7-2-8(3-9-4-12(21)20-14(7)9)13-10(16)5-19-6-11(13)22-15(17)18/h2-3,5-6,15H,4H2,1H3,(H,20,21)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459034
PNG
(CHEMBL4206704)
Show SMILES Cc1cccc(C)c1-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C16H15NO/c1-10-4-3-5-11(2)16(10)12-6-7-14-13(8-12)9-15(18)17-14/h3-8H,9H2,1-2H3,(H,17,18)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459035
PNG
(CHEMBL4207659 | US10611730, Example 20)
Show SMILES COc1cccc(Cl)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C14H11ClN2O2/c1-19-12-4-2-3-9(15)13(12)8-5-6-10-11(7-8)17-14(18)16-10/h2-7H,1H3,(H2,16,17,18)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459020
PNG
(CHEMBL4203681)
Show SMILES Cc1cc(cc2CC(=O)Nc12)-c1c(Cl)cncc1OC(F)(F)F
Show InChI InChI=1S/C15H10ClF3N2O2/c1-7-2-8(3-9-4-12(22)21-14(7)9)13-10(16)5-20-6-11(13)23-15(17,18)19/h2-3,5-6H,4H2,1H3,(H,21,22)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459033
PNG
(CHEMBL4211080 | US10611730, Example 36)
Show SMILES Cc1cccc(Cl)c1-c1ccc2[nH]c(=O)[nH]c2c1
Show InChI InChI=1S/C14H11ClN2O/c1-8-3-2-4-10(15)13(8)9-5-6-11-12(7-9)17-14(18)16-11/h2-7H,1H3,(H2,16,17,18)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit


(Homo sapiens (Human))
BDBM50459036
PNG
(CHEMBL4211865)
Show SMILES Cc1cc(cc2CC(=O)Nc12)-c1c(Cl)cccc1OC(F)(F)F
Show InChI InChI=1S/C16H11ClF3NO2/c1-8-5-9(6-10-7-13(22)21-15(8)10)14-11(17)3-2-4-12(14)23-16(18,19)20/h2-6H,7H2,1H3,(H,21,22)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma2 expressed in HEK293F cells assessed as blockade of glutamate-induced calcium flux by ca...


ACS Med Chem Lett 9: 821-826 (2018)


Article DOI: 10.1021/acsmedchemlett.8b00215
BindingDB Entry DOI: 10.7270/Q2ZW1PJ3
More data for this
Ligand-Target Pair