Found 105 hits of ic50 for UniProtKB: P14867 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 |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337263
(3-(2-chlorobenzyloxy)-2-(2-fluorophenyl)-2H-pyrazo...)Show SMILES Fc1ccccc1-n1nc2c(cnc3ccccc23)c1OCc1ccccc1Cl Show InChI InChI=1S/C23H15ClFN3O/c24-18-9-3-1-7-15(18)14-29-23-17-13-26-20-11-5-2-8-16(20)22(17)27-28(23)21-12-6-4-10-19(21)25/h1-13H,14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM84957
(CGS 9896 | CHEMBL20042)Show InChI InChI=1S/C16H10ClN3O/c17-10-5-7-11(8-6-10)20-16(21)13-9-18-14-4-2-1-3-12(14)15(13)19-20/h1-9,19H | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50290077
(CHEMBL73416 | N-[2-(4-Chloro-phenyl)-imidazo[1,2-a...)Show InChI InChI=1S/C19H20ClN3O/c1-3-6-18(24)22(2)13-16-19(14-8-10-15(20)11-9-14)21-17-7-4-5-12-23(16)17/h4-5,7-12H,3,6,13H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article
| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors) |
Bioorg Med Chem Lett 7: 2277-2282 (1997)
Article DOI: 10.1016/S0960-894X(97)00404-6 BindingDB Entry DOI: 10.7270/Q2BK1CB0 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50290077
(CHEMBL73416 | N-[2-(4-Chloro-phenyl)-imidazo[1,2-a...)Show InChI InChI=1S/C19H20ClN3O/c1-3-6-18(24)22(2)13-16-19(14-8-10-15(20)11-9-14)21-17-7-4-5-12-23(16)17/h4-5,7-12H,3,6,13H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article
| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors) |
Bioorg Med Chem Lett 7: 2277-2282 (1997)
Article DOI: 10.1016/S0960-894X(97)00404-6 BindingDB Entry DOI: 10.7270/Q2BK1CB0 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM98558
(US8492408, 7a)Show SMILES COc1ncccc1-c1cc(ccn1)-n1cnc2cc(ccc12)C(C)(C)O Show InChI InChI=1S/C21H20N4O2/c1-21(2,26)14-6-7-19-18(11-14)24-13-25(19)15-8-10-22-17(12-15)16-5-4-9-23-20(16)27-3/h4-13,26H,1-3H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 1.20 | n/a | n/a | n/a | n/a | n/a | n/a |
Aniona APS
US Patent
| Assay Description In vitro inhibition assay using GABA receptor. |
US Patent US8492408 (2013)
BindingDB Entry DOI: 10.7270/Q28K77QX |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50608946
(CHEMBL2008708) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| | n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50483961
(CHEMBL1795561)Show SMILES Br.OC(=O)CCCn1nc(ccc1=N)-c1ccc(OCc2cccc(c2)[N+]([O-])=O)cc1 Show InChI InChI=1S/C21H20N4O5/c22-20-11-10-19(23-24(20)12-2-5-21(26)27)16-6-8-18(9-7-16)30-14-15-3-1-4-17(13-15)25(28)29/h1,3-4,6-11,13,22H,2,5,12,14H2,(H,26,27) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 3 | n/a | n/a | n/a | n/a | n/a | n/a |
University College London
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current ... |
Bioorg Med Chem Lett 21: 4252-4 (2011)
Article DOI: 10.1016/j.bmcl.2011.05.067 BindingDB Entry DOI: 10.7270/Q2QR5101 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50608947
(CHEMBL5281056) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| | n/a | n/a | 3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50483959
(CHEMBL1795560)Show SMILES Br.COc1cccc(COc2ccc(cc2)-c2ccc(=N)n(CCCC(O)=O)n2)c1 Show InChI InChI=1S/C22H23N3O4/c1-28-19-5-2-4-16(14-19)15-29-18-9-7-17(8-10-18)20-11-12-21(23)25(24-20)13-3-6-22(26)27/h2,4-5,7-12,14,23H,3,6,13,15H2,1H3,(H,26,27) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 7 | n/a | n/a | n/a | n/a | n/a | n/a |
University College London
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current ... |
Bioorg Med Chem Lett 21: 4252-4 (2011)
Article DOI: 10.1016/j.bmcl.2011.05.067 BindingDB Entry DOI: 10.7270/Q2QR5101 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM98560
(US8492408, 7c)Show SMILES CC(C)(O)c1ccc2n(cnc2c1)-c1ccnc(c1)-c1ccncc1F Show InChI InChI=1S/C20H17FN4O/c1-20(2,26)13-3-4-19-18(9-13)24-12-25(19)14-5-8-23-17(10-14)15-6-7-22-11-16(15)21/h3-12,26H,1-2H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 7.5 | n/a | n/a | n/a | n/a | n/a | n/a |
Aniona APS
US Patent
| Assay Description In vitro inhibition assay using GABA receptor. |
US Patent US8492408 (2013)
BindingDB Entry DOI: 10.7270/Q28K77QX |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50537125
(CHEMBL1851667)Show InChI InChI=1S/C21H21N3O3/c22-20-13-12-19(23-24(20)14-4-7-21(25)26)17-8-10-18(11-9-17)27-15-16-5-2-1-3-6-16/h1-3,5-6,8-13,22H,4,7,14-15H2,(H,25,26) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA(A) receptor expressed in human tsA201 cells assessed as inhibition of GABA-induced membrane pote... |
J Med Chem 62: 2798-2813 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00131 BindingDB Entry DOI: 10.7270/Q2D2225V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50483958
(CHEMBL1795348)Show SMILES Br.OC(=O)CCCn1nc(ccc1=N)-c1ccc(OCc2ccccc2)cc1 Show InChI InChI=1S/C21H21N3O3/c22-20-13-12-19(23-24(20)14-4-7-21(25)26)17-8-10-18(11-9-17)27-15-16-5-2-1-3-6-16/h1-3,5-6,8-13,22H,4,7,14-15H2,(H,25,26) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 11 | n/a | n/a | n/a | n/a | n/a | n/a |
University College London
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current ... |
Bioorg Med Chem Lett 21: 4252-4 (2011)
Article DOI: 10.1016/j.bmcl.2011.05.067 BindingDB Entry DOI: 10.7270/Q2QR5101 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM26266
(Ambien | CHEMBL911 | Dalparan | N,N-dimethyl-2-[6-...)Show InChI InChI=1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank KEGG PC cid PC sid PDB UniChem
Patents
Similars
| DrugBank PDB Article
| n/a | n/a | 14 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Inhibition of [3H]-Flumazenil binding to recombinant GABA-A receptor alpha-1 subunit in cerebellum |
Bioorg Med Chem Lett 7: 2277-2282 (1997)
Article DOI: 10.1016/S0960-894X(97)00404-6 BindingDB Entry DOI: 10.7270/Q2BK1CB0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378769
(CHEMBL1204074)Show InChI InChI=1S/C20H21N3O/c24-23-20(19(14-22-23)16-9-11-21-12-10-16)18-8-4-7-17(13-18)15-5-2-1-3-6-15/h1-8,13-14,16,21,24H,9-12H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 24 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA(A) receptor expressed in human tsA201 cells assessed as inhibition of GABA-induced membrane pote... |
J Med Chem 62: 2798-2813 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00131 BindingDB Entry DOI: 10.7270/Q2D2225V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378769
(CHEMBL1204074)Show InChI InChI=1S/C20H21N3O/c24-23-20(19(14-22-23)16-9-11-21-12-10-16)18-8-4-7-17(13-18)15-5-2-1-3-6-15/h1-8,13-14,16,21,24H,9-12H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 24 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells by FMP red assay |
J Med Chem 53: 3417-21 (2010)
Article DOI: 10.1021/jm100106r BindingDB Entry DOI: 10.7270/Q2GF0VFM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM98561
(US8492408, 7d)Show SMILES CC(C)(O)c1ccc2n(cnc2c1)-c1ccnc(c1)-c1ccncc1C#N Show InChI InChI=1S/C21H17N5O/c1-21(2,27)15-3-4-20-19(9-15)25-13-26(20)16-5-8-24-18(10-16)17-6-7-23-12-14(17)11-22/h3-10,12-13,27H,1-2H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 26 | n/a | n/a | n/a | n/a | n/a | n/a |
Aniona APS
US Patent
| Assay Description In vitro inhibition assay using GABA receptor. |
US Patent US8492408 (2013)
BindingDB Entry DOI: 10.7270/Q28K77QX |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50329649
(1-phenylethyl 9H-pyrido[3,4-b]indole-3-carboxylate...)Show InChI InChI=1S/C20H16N2O2/c1-13(14-7-3-2-4-8-14)24-20(23)18-11-16-15-9-5-6-10-17(15)22-19(16)12-21-18/h2-13,22H,1H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| | n/a | n/a | 34 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM98559
(US8492408, 7b)Show SMILES CC(C)(O)c1ccc2n(cnc2c1)-c1ccnc(c1)-c1cccnc1Cl Show InChI InChI=1S/C20H17ClN4O/c1-20(2,26)13-5-6-18-17(10-13)24-12-25(18)14-7-9-22-16(11-14)15-4-3-8-23-19(15)21/h3-12,26H,1-2H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| US Patent
| n/a | n/a | 38 | n/a | n/a | n/a | n/a | n/a | n/a |
Aniona APS
US Patent
| Assay Description In vitro inhibition assay using GABA receptor. |
US Patent US8492408 (2013)
BindingDB Entry DOI: 10.7270/Q28K77QX |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50483960
(CHEMBL1795562)Show InChI InChI=1S/C17H17N3O3/c1-2-12-23-14-7-5-13(6-8-14)15-9-10-16(18)20(19-15)11-3-4-17(21)22/h1,5-10,18H,3-4,11-12H2,(H,21,22) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 40 | n/a | n/a | n/a | n/a | n/a | n/a |
University College London
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current ... |
Bioorg Med Chem Lett 21: 4252-4 (2011)
Article DOI: 10.1016/j.bmcl.2011.05.067 BindingDB Entry DOI: 10.7270/Q2QR5101 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM26266
(Ambien | CHEMBL911 | Dalparan | N,N-dimethyl-2-[6-...)Show InChI InChI=1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank KEGG PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article
| n/a | n/a | 46 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors) |
Bioorg Med Chem Lett 7: 2277-2282 (1997)
Article DOI: 10.1016/S0960-894X(97)00404-6 BindingDB Entry DOI: 10.7270/Q2BK1CB0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337265
(3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-6,7,8,9-t...)Show SMILES Clc1ccc(cc1)-n1nc2c3CCCCc3ncc2c1OCc1ccccc1Cl Show InChI InChI=1S/C23H19Cl2N3O/c24-16-9-11-17(12-10-16)28-23(29-14-15-5-1-3-7-20(15)25)19-13-26-21-8-4-2-6-18(21)22(19)27-28/h1,3,5,7,9-13H,2,4,6,8,14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 46 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337271
(2-(4-chlorophenyl)-3-(4-fluorobenzyloxy)-6,7,8,9-t...)Show SMILES Fc1ccc(COc2n(nc3c4CCCCc4ncc23)-c2ccc(Cl)cc2)cc1 Show InChI InChI=1S/C23H19ClFN3O/c24-16-7-11-18(12-8-16)28-23(29-14-15-5-9-17(25)10-6-15)20-13-26-21-4-2-1-3-19(21)22(20)27-28/h5-13H,1-4,14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337264
(2-(benzo[d][1,3]dioxol-5-yl)-3-(2-chlorobenzyloxy)...)Show SMILES Clc1ccccc1COc1n(nc2c1cnc1ccccc21)-c1ccc2OCOc2c1 Show InChI InChI=1S/C24H16ClN3O3/c25-19-7-3-1-5-15(19)13-29-24-18-12-26-20-8-4-2-6-17(20)23(18)27-28(24)16-9-10-21-22(11-16)31-14-30-21/h1-12H,13-14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 50 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337274
(3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-2H-pyrazo...)Show SMILES Clc1ccc(cc1)-n1nc2c(cnc3ccccc23)c1OCc1ccccc1Cl Show InChI InChI=1S/C23H15Cl2N3O/c24-16-9-11-17(12-10-16)28-23(29-14-15-5-1-3-7-20(15)25)19-13-26-21-8-4-2-6-18(21)22(19)27-28/h1-13H,14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 64 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337270
(2-(4-chlorophenyl)-3-(2-fluorobenzyloxy)-6,7,8,9-t...)Show SMILES Fc1ccccc1COc1n(nc2c3CCCCc3ncc12)-c1ccc(Cl)cc1 Show InChI InChI=1S/C23H19ClFN3O/c24-16-9-11-17(12-10-16)28-23(29-14-15-5-1-3-7-20(15)25)19-13-26-21-8-4-2-6-18(21)22(19)27-28/h1,3,5,7,9-13H,2,4,6,8,14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 64 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337268
(3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-8,8-dimet...)Show SMILES CC1(C)CCc2ncc3c(OCc4ccccc4Cl)n(nc3c2C1)-c1ccc(Cl)cc1 Show InChI InChI=1S/C25H23Cl2N3O/c1-25(2)12-11-22-19(13-25)23-20(14-28-22)24(31-15-16-5-3-4-6-21(16)27)30(29-23)18-9-7-17(26)8-10-18/h3-10,14H,11-13,15H2,1-2H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 67 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337272
(2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-2H-pyraz...)Show InChI InChI=1S/C20H16ClN3O/c21-14-7-9-15(10-8-14)24-20(25-12-13-5-6-13)17-11-22-18-4-2-1-3-16(18)19(17)23-24/h1-4,7-11,13H,5-6,12H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 74 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50520683
(CHEMBL4476621)Show InChI InChI=1S/C14H11Cl2N3O2S/c15-10-6-5-8(7-11(10)16)17-14(22)19-18-13(21)9-3-1-2-4-12(9)20/h1-7,20H,(H,18,21)(H2,17,19,22) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 75 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ Catholique de Louvain (UCLouvain)
Curated by ChEMBL
| Assay Description Displacement of [3H]muscimol from recombinant human GABAalpha1beta2gamma2 measured after 120 mins by scintillation counting method |
Eur J Med Chem 159: 324-338 (2018)
Article DOI: 10.1016/j.ejmech.2018.09.067 BindingDB Entry DOI: 10.7270/Q2VM4GND |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50208721
(4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol ...)Show InChI InChI=1S/C20H20N2O2/c23-20-18(19(24-22-20)15-9-11-21-12-10-15)17-8-4-7-16(13-17)14-5-2-1-3-6-14/h1-8,13,15,21H,9-12H2,(H,22,23) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 78 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells by FMP red assay |
J Med Chem 53: 3417-21 (2010)
Article DOI: 10.1021/jm100106r BindingDB Entry DOI: 10.7270/Q2GF0VFM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337275
(2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-6,7,8,9-...)Show InChI InChI=1S/C20H20ClN3O/c21-14-7-9-15(10-8-14)24-20(25-12-13-5-6-13)17-11-22-18-4-2-1-3-16(18)19(17)23-24/h7-11,13H,1-6,12H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 94 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM26266
(Ambien | CHEMBL911 | Dalparan | N,N-dimethyl-2-[6-...)Show InChI InChI=1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank KEGG PC cid PC sid PDB UniChem
Patents
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| DrugBank PDB Article
| n/a | n/a | 130 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB r... |
Bioorg Med Chem Lett 7: 2277-2282 (1997)
Article DOI: 10.1016/S0960-894X(97)00404-6 BindingDB Entry DOI: 10.7270/Q2BK1CB0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337277
(2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-8-(1H-im...)Show SMILES Clc1ccc(cc1)-n1nc2c(cnc3ccc(cc23)-n2ccnc2)c1OCC1CC1 Show InChI InChI=1S/C23H18ClN5O/c24-16-3-5-17(6-4-16)29-23(30-13-15-1-2-15)20-12-26-21-8-7-18(28-10-9-25-14-28)11-19(21)22(20)27-29/h3-12,14-15H,1-2,13H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 134 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378770
(CHEMBL1202335)Show InChI InChI=1S/C14H17N3O/c18-17-14(12-4-2-1-3-5-12)13(10-16-17)11-6-8-15-9-7-11/h1-5,10-11,15,18H,6-9H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 150 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells by FMP red assay |
J Med Chem 53: 3417-21 (2010)
Article DOI: 10.1021/jm100106r BindingDB Entry DOI: 10.7270/Q2GF0VFM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50097413
(CHEMBL3586473)Show SMILES COc1cccc(F)c1C1=NCc2cnc(Nc3ccc(cc3)C(O)=O)nc2-c2ccc(Cl)cc12 |t:10| Show InChI InChI=1S/C26H18ClFN4O3/c1-35-21-4-2-3-20(28)22(21)24-19-11-16(27)7-10-18(19)23-15(12-29-24)13-30-26(32-23)31-17-8-5-14(6-9-17)25(33)34/h2-11,13H,12H2,1H3,(H,33,34)(H,30,31,32) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 150 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
Curated by ChEMBL
| Assay Description Binding affinity to GABAA alpha-1 benzodiazepine binding site (unknown origin) |
ACS Med Chem Lett 6: 630-4 (2015)
Article DOI: 10.1021/ml500409n BindingDB Entry DOI: 10.7270/Q2WS8W1V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337269
(3-(4-chlorobenzyloxy)-2-(4-chlorophenyl)-6,7,8,9-t...)Show SMILES Clc1ccc(COc2n(nc3c4CCCCc4ncc23)-c2ccc(Cl)cc2)cc1 Show InChI InChI=1S/C23H19Cl2N3O/c24-16-7-5-15(6-8-16)14-29-23-20-13-26-21-4-2-1-3-19(21)22(20)27-28(23)18-11-9-17(25)10-12-18/h5-13H,1-4,14H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 157 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378760
(CHEMBL1202340)Show InChI InChI=1S/C19H21N3O/c23-22-13-18(16-7-9-20-10-8-16)19(21-22)12-14-5-6-15-3-1-2-4-17(15)11-14/h1-6,11,13,16,20,23H,7-10,12H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 170 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells by FMP red assay |
J Med Chem 53: 3417-21 (2010)
Article DOI: 10.1021/jm100106r BindingDB Entry DOI: 10.7270/Q2GF0VFM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378763
(CHEMBL1204077)Show InChI InChI=1S/C20H21N3O/c24-23-14-19(16-9-11-21-12-10-16)20(22-23)18-8-4-7-17(13-18)15-5-2-1-3-6-15/h1-8,13-14,16,21,24H,9-12H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins... |
J Med Chem 56: 6536-40 (2013)
Article DOI: 10.1021/jm4006466 BindingDB Entry DOI: 10.7270/Q2K35XKM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378763
(CHEMBL1204077)Show InChI InChI=1S/C20H21N3O/c24-23-14-19(16-9-11-21-12-10-16)20(22-23)18-8-4-7-17(13-18)15-5-2-1-3-6-15/h1-8,13-14,16,21,24H,9-12H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells by FMP red assay |
J Med Chem 53: 3417-21 (2010)
Article DOI: 10.1021/jm100106r BindingDB Entry DOI: 10.7270/Q2GF0VFM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50493007
(CHEMBL2420450)Show SMILES On1cc(C2CCNCC2)c(n1)-c1cn(Cc2ccccc2)c(n1)-c1ccccc1 Show InChI InChI=1S/C24H25N5O/c30-29-16-21(19-11-13-25-14-12-19)23(27-29)22-17-28(15-18-7-3-1-4-8-18)24(26-22)20-9-5-2-6-10-20/h1-10,16-17,19,25,30H,11-15H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins... |
J Med Chem 56: 6536-40 (2013)
Article DOI: 10.1021/jm4006466 BindingDB Entry DOI: 10.7270/Q2K35XKM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378763
(CHEMBL1204077)Show InChI InChI=1S/C20H21N3O/c24-23-14-19(16-9-11-21-12-10-16)20(22-23)18-8-4-7-17(13-18)15-5-2-1-3-6-15/h1-8,13-14,16,21,24H,9-12H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA(A) receptor expressed in human tsA201 cells assessed as inhibition of GABA-induced membrane pote... |
J Med Chem 62: 2798-2813 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00131 BindingDB Entry DOI: 10.7270/Q2D2225V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50493007
(CHEMBL2420450)Show SMILES On1cc(C2CCNCC2)c(n1)-c1cn(Cc2ccccc2)c(n1)-c1ccccc1 Show InChI InChI=1S/C24H25N5O/c30-29-16-21(19-11-13-25-14-12-19)23(27-29)22-17-28(15-18-7-3-1-4-8-18)24(26-22)20-9-5-2-6-10-20/h1-10,16-17,19,25,30H,11-15H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 214 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins... |
J Med Chem 56: 6536-40 (2013)
Article DOI: 10.1021/jm4006466 BindingDB Entry DOI: 10.7270/Q2K35XKM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50001572
((gabazine)4-[6-Imino-3-(4-methoxy-phenyl)-6H-pyrid...)Show InChI InChI=1S/C15H17N3O3/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20/h4-9,16H,2-3,10H2,1H3,(H,19,20) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE KEGG PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 240 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA(A) receptor expressed in human tsA201 cells assessed as inhibition of GABA-induced membrane pote... |
J Med Chem 62: 2798-2813 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00131 BindingDB Entry DOI: 10.7270/Q2D2225V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50001572
((gabazine)4-[6-Imino-3-(4-methoxy-phenyl)-6H-pyrid...)Show InChI InChI=1S/C15H17N3O3/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20/h4-9,16H,2-3,10H2,1H3,(H,19,20) | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL MCE KEGG PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 240 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins... |
J Med Chem 56: 6536-40 (2013)
Article DOI: 10.1021/jm4006466 BindingDB Entry DOI: 10.7270/Q2K35XKM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50337266
(3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-2,6,7,8,9...)Show SMILES Clc1ccc(cc1)-n1nc2c3CCCCCc3ncc2c1OCc1ccccc1Cl Show InChI InChI=1S/C24H21Cl2N3O/c25-17-10-12-18(13-11-17)29-24(30-15-16-6-4-5-8-21(16)26)20-14-27-22-9-3-1-2-7-19(22)23(20)28-29/h4-6,8,10-14H,1-3,7,9,15H2 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 242 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for BioMedical Research
Curated by ChEMBL
| Assay Description Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells |
Bioorg Med Chem Lett 21: 1523-6 (2011)
Article DOI: 10.1016/j.bmcl.2010.12.107 BindingDB Entry DOI: 10.7270/Q289164V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM31093
(4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-py...)Show SMILES OC(=O)c1ccc(Nc2ncc3CN=C(c4cc(Cl)ccc4-c3n2)c2c(F)cccc2F)cc1 |c:13| Show InChI InChI=1S/C25H15ClF2N4O2/c26-15-6-9-17-18(10-15)23(21-19(27)2-1-3-20(21)28)29-11-14-12-30-25(32-22(14)17)31-16-7-4-13(5-8-16)24(33)34/h1-10,12H,11H2,(H,33,34)(H,30,31,32) | PDB
Reactome pathway KEGG
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| n/a | n/a | 330 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
Curated by ChEMBL
| Assay Description Binding affinity to GABAA alpha-1 benzodiazepine binding site (unknown origin) |
ACS Med Chem Lett 6: 630-4 (2015)
Article DOI: 10.1021/ml500409n BindingDB Entry DOI: 10.7270/Q2WS8W1V |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50001572
((gabazine)4-[6-Imino-3-(4-methoxy-phenyl)-6H-pyrid...)Show InChI InChI=1S/C15H17N3O3/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20/h4-9,16H,2-3,10H2,1H3,(H,19,20) | PDB
UniProtKB/SwissProt
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CHEMBL MCE KEGG PC cid PC sid UniChem
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| n/a | n/a | 349 | n/a | n/a | n/a | n/a | n/a | n/a |
University College London
Curated by ChEMBL
| Assay Description Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current ... |
Bioorg Med Chem Lett 21: 4252-4 (2011)
Article DOI: 10.1016/j.bmcl.2011.05.067 BindingDB Entry DOI: 10.7270/Q2QR5101 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50244157
(CHEMBL458317 | N-(4-chlorophenyl)-5-(2-(methylthio...)Show SMILES CSc1nccc(n1)-c1ccc(s1)S(=O)(=O)Nc1ccc(Cl)cc1 Show InChI InChI=1S/C15H12ClN3O2S3/c1-22-15-17-9-8-12(18-15)13-6-7-14(23-13)24(20,21)19-11-4-2-10(16)3-5-11/h2-9,19H,1H3 | PDB
Reactome pathway KEGG
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DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL PC cid PC sid UniChem
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| n/a | n/a | 470 | n/a | n/a | n/a | n/a | n/a | n/a |
Moltech Corporation
Curated by ChEMBL
| Assay Description Displacement of [3H]Ro15-4513 from GABAA alpha-1-beta-2-gamma-2 receptor expressed in Sf9 baculovirus system |
J Med Chem 51: 3788-803 (2008)
Article DOI: 10.1021/jm701433b BindingDB Entry DOI: 10.7270/Q2FQ9XH6 |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM126720
(US8778932, 31)Show SMILES CC1=NN=C(c2cc3c(cccc3s2)C(F)(F)F)c2cc3oc(=O)[nH]c3cc2C1 |t:1,3| Show InChI InChI=1S/C20H12F3N3O2S/c1-9-5-10-6-14-15(28-19(27)24-14)7-11(10)18(26-25-9)17-8-12-13(20(21,22)23)3-2-4-16(12)29-17/h2-4,6-8H,5H2,1H3,(H,24,27) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 479 | n/a | n/a | n/a | n/a | n/a | n/a |
Jain University
Curated by ChEMBL
| Assay Description Antagonist activity at human GABA-A alpha1 receptor expressed in HEK293 cell membranes assessed as inhibition of GABA-induced response preincubated f... |
Eur J Med Chem 138: 1002-1033 (2017)
Article DOI: 10.1016/j.ejmech.2017.07.038 BindingDB Entry DOI: 10.7270/Q2C24ZZC |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
(Homo sapiens (Human)) | BDBM50378771
(CHEMBL1204073)Show InChI InChI=1S/C19H20BrN3O/c20-19-15(6-5-13-3-1-2-4-16(13)19)11-18-17(12-22-23(18)24)14-7-9-21-10-8-14/h1-6,12,14,21,24H,7-11H2 | PDB
UniProtKB/SwissProt
antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 480 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Antagonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells by FMP red assay |
J Med Chem 53: 3417-21 (2010)
Article DOI: 10.1021/jm100106r BindingDB Entry DOI: 10.7270/Q2GF0VFM |
More data for this Ligand-Target Pair | |
Gamma-aminobutyric acid receptor subunit alpha-1
(Homo sapiens (Human)) | BDBM50277545
(4-(9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[...)Show SMILES COc1cc(Nc2ncc3CN=C(c4cc(Cl)ccc4-c3n2)c2c(F)cccc2OC)ccc1C(O)=O |c:11| Show InChI InChI=1S/C27H20ClFN4O4/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 490 | n/a | n/a | n/a | n/a | n/a | n/a |
Takeda Pharmaceuticals International Co. , 40 Landsdowne Street, Cambridge, Massachusetts 02139, United States.
Curated by ChEMBL
| Assay Description Binding affinity to GABAA alpha-1 benzodiazepine binding site (unknown origin) |
ACS Med Chem Lett 6: 630-4 (2015)
Article DOI: 10.1021/ml500409n BindingDB Entry DOI: 10.7270/Q2WS8W1V |
More data for this Ligand-Target Pair | |