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Compile Data Set for Download or QSAR

Found 20 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-8 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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n/an/a 0.200n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 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/TARPgamma8 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-8 subunit


(Homo sapiens (Human))
BDBM50459021
PNG
(CHEMBL4212408 | US10611730, Example 76)
Show SMILES FC(F)(F)Oc1cccc(Cl)c1-c1ccc2[nH]c(=O)sc2c1
Show InChI InChI=1S/C14H7ClF3NO2S/c15-8-2-1-3-10(21-14(16,17)18)12(8)7-4-5-9-11(6-7)22-13(20)19-9/h1-6H,(H,19,20)
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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 subunit


(Homo sapiens (Human))
BDBM50459031
PNG
(CHEMBL4216837)
Show SMILES Fc1cc(cc2CC(=O)Nc12)-c1c(Cl)cccc1OC(F)(F)F
Show InChI InChI=1S/C15H8ClF4NO2/c16-9-2-1-3-11(23-15(18,19)20)13(9)7-4-8-6-12(22)21-14(8)10(17)5-7/h1-5H,6H2,(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/TARPgamma8 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-8 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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n/an/a 6.30n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 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/TARPgamma8 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-8 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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Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 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/TARPgamma8 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-8 subunit


(Homo sapiens (Human))
BDBM50459019
PNG
(CHEMBL4207505)
Show SMILES FC(F)(F)Oc1cccc(Cl)c1-c1ccc2NC(=O)Cc2c1
Show InChI InChI=1S/C15H9ClF3NO2/c16-10-2-1-3-12(22-15(17,18)19)14(10)8-4-5-11-9(6-8)7-13(21)20-11/h1-6H,7H2,(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/TARPgamma8 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-8 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/TARPgamma8 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-8 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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n/an/a 50n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 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/TARPgamma8 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-8 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/TARPgamma8 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-8 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/TARPgamma8 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-8 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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Sanford Burnham Prebys Medical Discovery Institute

Curated by ChEMBL


Assay Description
Negative allosteric modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 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/TARPgamma8 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-8 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/TARPgamma8 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-8 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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n/an/a 398n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 subunit


(Homo sapiens (Human))
BDBM50459024
PNG
(CHEMBL4212562)
Show SMILES FC(F)(F)Oc1cccc(Cl)c1-c1ccc2[nH]c(=O)oc2c1
Show InChI InChI=1S/C14H7ClF3NO3/c15-8-2-1-3-10(22-14(16,17)18)12(8)7-4-5-9-11(6-7)21-13(20)19-9/h1-6H,(H,19,20)
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n/an/a 2.51E+3n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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-8 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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n/an/a 2.51E+3n/an/an/an/an/an/a



Janssen Research & Development L.L.C.

Curated by ChEMBL


Assay Description
Modulation of recombinant human GluA1 flop isoform/TARPgamma8 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