Target
P2X purinoceptor 7
Ligand
BDBM203332
Substrate
n/a
Meas. Tech.
Ca2+ Flux Assay
pH
7.4±n/a
Ki
3.20±n/a nM
IC50
14±n/a nM
Comments
extracted
Citation
 Letavic, MARudolph, DA P2X7 modulators US Patent  US9540388 Publication Date 1/10/2017 
Target
Name:
P2X purinoceptor 7
Synonyms:
ATP receptor | P2RX7 | P2RX7_HUMAN | P2X purinoceptor 7 (P2RX7) | P2X purinoceptor 7 (P2X7) | P2X7 | P2Z receptor | Purinergic receptor
Type:
Protein
Mol. Mass.:
68602.85
Organism:
Homo sapiens (Human)
Description:
Q99572
Residue:
595
Sequence:
MPACCSCSDVFQYETNKVTRIQSMNYGTIKWFFHVIIFSYVCFALVSDKLYQRKEPVISSVHTKVKGIAEVKEEIVENGVKKLVHSVFDTADYTFPLQGNSFFVMTNFLKTEGQEQRLCPEYPTRRTLCSSDRGCKKGWMDPQSKGIQTGRCVVYEGNQKTCEVSAWCPIEAVEEAPRPALLNSAENFTVLIKNNIDFPGHNYTTRNILPGLNITCTFHKTQNPQCPIFRLGDIFRETGDNFSDVAIQGGIMGIEIYWDCNLDRWFHHCRPKYSFRRLDDKTTNVSLYPGYNFRYAKYYKENNVEKRTLIKVFGIRFDILVFGTGGKFDIIQLVVYIGSTLSYFGLAAVFIDFLIDTYSSNCCRSHIYPWCKCCQPCVVNEYYYRKKCESIVEPKPTLKYVSFVDESHIRMVNQQLLGRSLQDVKGQEVPRPAMDFTDLSRLPLALHDTPPIPGQPEEIQLLRKEATPRSRDSPVWCQCGSCLPSQLPESHRCLEELCCRKKPGACITTSELFRKLVLSRHVLQFLLLYQEPLLALDVDSTNSRLRHCAYRCYATWRFGSQDMADFAILPSCCRWRIRKEFPKSEGQYSGFKSPY
  
Inhibitor
Name:
BDBM203332
Synonyms:
(6r,10s)-11-{[2-methyl-3-(trifluoromethyl)phenyl]carbonyl}-3-pyridin-2-yl-5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocine | US10053462, 201 | US9540388, 201
Type:
Small organic molecule
Emp. Form.:
C22H20F3N5O
Mol. Mass.:
427.4223
SMILES:
Cc1c(cccc1C(F)(F)F)C(=O)N1[C@H]2CCC[C@@H]1c1nnc(-c3ccccn3)n1C2 |r,THB:11:13:19.29.30:15.16.17|
Structure:
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