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Target
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit
Ligand
BDBM50459030
Substrate
n/a
Meas. Tech.
ChEMBL_1765298 (CHEMBL4200545)
IC50
<10000±n/a nM
Citation
 Ravula, S; Savall, BM; Wu, N; Lord, B; Coe, K; Wang, K; Seierstad, M; Swanson, DM; Ziff, J; Nguyen, M; Leung, P; Rynberg, R; La, D; Pippel, DJ; Koudriakova, T; Lovenberg, TW; Carruthers, NI; Maher, MP; Ameriks, MK Lead Optimization of 5-Aryl Benzimidazolone- and Oxindole-Based AMPA Receptor Modulators Selective for TARP ?-8. ACS Med Chem Lett 9:821-826 (2018) [PubMed]  Article 
Target
Name:
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit
Synonyms:
GRIA1/CACNG2
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1839473
Components:
This complex has 2 components.
Component 1
Name:
Glutamate receptor 1
Synonyms:
AMPA-selective glutamate receptor 1 | GLUH1 | GLUR1 | GRIA1 | GRIA1_HUMAN | GluR-1 | GluR-A | GluR-K1 | Glutamate AMPA 1 | Glutamate receptor 1 | Glutamate receptor AMPA 1/2 | Glutamate receptor ionotropic AMPA | Glutamate receptor ionotropic, AMPA 1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
101512.92
Organism:
Homo sapiens (Human)
Description:
Glutamate AMPA 1 GRIA1 HUMAN::P42261
Residue:
906
Sequence:
MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMPLGATGL
  
Component 2
Name:
Voltage-dependent calcium channel gamma-2 subunit
Synonyms:
CACNG2 | CCG2_HUMAN | Neuronal voltage-gated calcium channel gamma-2 subunit | TARP gamma-2 | Transmembrane AMPAR regulatory protein gamma-2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
35977.54
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
323
Sequence:
MGLFDRGVQMLLTTVGAFAAFSLMTIAVGTDYWLYSRGVCKTKSVSENETSKKNEEVMTHSGLWRTCCLEGNFKGLCKQIDHFPEDADYEADTAEYFLRAVRASSIFPILSVILLFMGGLCIAASEFYKTRHNIILSAGIFFVSAGLSNIIGIIVYISANAGDPSKSDSKKNSYSYGWSFYFGALSFIIAEMVGVLAVHMFIDRHKQLRATARATDYLQASAITRIPSYRYRYQRRSRSSSRSTEPSHSRDASPVGIKGFNTLPSTEISMYTLSRDPLKAATTPTATYNSDRDNSFLQVHNCIQKENKDSLHSNTANRRTTPV
  
Inhibitor
Name:
BDBM50459030
Synonyms:
CHEMBL4207238 | US10611730, Example 124
Type:
Small organic molecule
Emp. Form.:
C15H10ClN3O
Mol. Mass.:
283.712
SMILES:
Clc1cccc(CC#N)c1-c1ccc2[nH]c(=O)[nH]c2c1
Structure:
Search PDB for entries with ligand similarity: