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Target
P2X purinoceptor 7
Ligand
BDBM254218
Substrate
n/a
Meas. Tech.
Ca2+ flux assay
pH
7.4±n/a
IC50
128±n/a nM
Comments
extracted
Citation
 Alcazar Vaca, MJ; Allison, BD; Andres Gil, JI; Chrovian, CC; Coate, HR; De Angelis, M; Deng, X; Dvorak, CA; Gelin, CF; Letavic, MA; Liang, JT; Mani, NS; Rech, JC; Savall, BM; Soyode-Johnson, A; Stenne, BM; Swanson, DM; Wall, JL P2X7 modulators and methods of use US Patent  US10112937 Publication Date 10/30/2018 
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:
BDBM254218
Synonyms:
US10112937, Example 103 | US10150765, Example 103 | US10703749, Example 103 | US9464084, 103
Type:
Small organic molecule
Emp. Form.:
C20H17Cl2N3O
Mol. Mass.:
386.274
SMILES:
Cn1nc(c2CCN(Cc12)C(=O)c1cccc(Cl)c1Cl)-c1ccccc1
Structure:
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