Reaction Details Report a problem with these data
Target
Voltage-dependent calcium channel gamma-8 subunit
Ligand
BDBM288217
Substrate
n/a
Meas. Tech.
Calcium Flux Assay
pH
7.4±n/a
IC50
0.398±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:
BDBM288217
Synonyms:
5-(7-Chloro-1H-indazol-5-yl)-2-ethyl-8-methyl-6-(trifluoromethyl)- | US10087185, Example 35
Type:
Small organic molecule
Emp. Form.:
C17H13ClF3N5
Mol. Mass.:
379.767
SMILES:
CCc1nc2c(C)cc(c(-c3cc(Cl)c4[nH]ncc4c3)n2n1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: