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Target
Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit
Ligand
BDBM426135
Substrate
n/a
Meas. Tech.
ChEMBL_1839473 (CHEMBL4339688)
IC50
0.100000±n/a nM
Citation
 Savall, BM; Wu, D; Swanson, DM; Seierstad, M; Wu, N; Vives Martinez, J; García Olmos, B; Lord, B; Coe, K; Koudriakova, T; Lovenberg, TW; Carruthers, NI; Maher, MP; Ameriks, MK Discovery of Imidazo[1,2- ACS Med Chem Lett 10:267-272 (2019) [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:
BDBM426135
Synonyms:
5-[2-(4-Fluorophenyl)-8-(4-fluoro-1-piperidyl)imidazo[1,2-a]pyrazin-3- | US10513523, Example 74
Type:
Small organic molecule
Emp. Form.:
C25H21F2N5O
Mol. Mass.:
445.4639
SMILES:
FC1CCN(CC1)c1nccn2c(c(nc12)-c1ccc(F)cc1)-c1ccc2NC(=O)Cc2c1
Structure:
Search PDB for entries with ligand similarity: