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Target
Voltage-dependent calcium channel gamma-8 subunit
Ligand
BDBM288252
Substrate
n/a
Meas. Tech.
Calcium Flux Assay
pH
7.4±n/a
IC50
0.063±n/a nM
Comments
extracted
Citation
 Ameriks, MK; Gyuris, M; Laforteza, BN; Lebold, TP; Meyer, ST; Ravula, S; Savall, BM; Shireman, BT; Wade, WS; Gerencsér, J Fused bicylic pyridine compounds and their use as AMPA receptor modulators US Patent  US10087185 Publication Date 10/2/2018 
Target
Name:
Voltage-dependent calcium channel gamma-8 subunit
Synonyms:
CACNG6 | CACNG8 | CCG8_HUMAN | Neuronal voltage-gated calcium channel gamma-8 subunit | TARP gamma-8 | Transmembrane AMPAR regulatory protein gamma-8
Type:
Enzyme Catalytic Domain
Mol. Mass.:
43326.96
Organism:
Homo sapiens (Human)
Description:
Q8WXS5
Residue:
425
Sequence:
MESLKRWNEERGLWCEKGVQVLLTTVGAFAAFGLMTIAISTDYWLYTRALICNTTNLTAGGDDGTPHRGGGGASEKKDPGGLTHSGLWRICCLEGLKRGVCVKINHFPEDTDYDHDSAEYLLRVVRASSIFPILSAILLLLGGVCVAASRVYKSKRNIILGAGILFVAAGLSNIIGVIVYISANAGEPGPKRDEEKKNHYSYGWSFYFGGLSFILAEVIGVLAVNIYIERSREAHCQSRSDLLKAGGGAGGSGGSGPSAILRLPSYRFRYRRRSRSSSRSSEPSPSRDASPGGPGGPGFASTDISMYTLSRDPSKGSVAAGLAGAGGGGGGAVGAFGGAAGGAGGGGGGGGGAGAERDRGGASGFLTLHNAFPKEAGGGVTVTVTGPPAPPAPAPPAPSAPAPGTLAKEAAASNTNTLNRKTTPV
  
Inhibitor
Name:
BDBM288252
Synonyms:
7-Chloro-5-(2-cyclopropyl-6-(trifluoromethyl)pyrazolo[1,5-a]pyridin- | US10087185, Example 118 | US10087185, Example 70
Type:
Small organic molecule
Emp. Form.:
C18H12ClF3N4
Mol. Mass.:
376.763
SMILES:
FC(F)(F)c1ccc2cc(nn2c1-c1cc(Cl)c2[nH]ncc2c1)C1CC1
Structure:
Search PDB for entries with ligand similarity: