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TargetP2X purinoceptor 7
LigandBDBM254160
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1616309 (CHEMBL3858378)
Ki 7.0±n/a nM
Citation Swanson, DMSavall, BMCoe, KJSchoetens, FKoudriakova, TSkaptason, JWall, JRech, JDeng, XDe Angelis, MEverson, ALord, BWang, QAo, HScott, BSepassi, KLovenberg, TWCarruthers, NIBhattacharya, ALetavic, MA Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. J Med Chem59:8535-48 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
P2X purinoceptor 7
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:
MPACCSCSDVFQYETNKVTRIQSMNYGTIKWFFHVIIFSYVCFALVSDKLYQRKEPVISS
VHTKVKGIAEVKEEIVENGVKKLVHSVFDTADYTFPLQGNSFFVMTNFLKTEGQEQRLCP
EYPTRRTLCSSDRGCKKGWMDPQSKGIQTGRCVVYEGNQKTCEVSAWCPIEAVEEAPRPA
LLNSAENFTVLIKNNIDFPGHNYTTRNILPGLNITCTFHKTQNPQCPIFRLGDIFRETGD
NFSDVAIQGGIMGIEIYWDCNLDRWFHHCRPKYSFRRLDDKTTNVSLYPGYNFRYAKYYK
ENNVEKRTLIKVFGIRFDILVFGTGGKFDIIQLVVYIGSTLSYFGLAAVFIDFLIDTYSS
NCCRSHIYPWCKCCQPCVVNEYYYRKKCESIVEPKPTLKYVSFVDESHIRMVNQQLLGRS
LQDVKGQEVPRPAMDFTDLSRLPLALHDTPPIPGQPEEIQLLRKEATPRSRDSPVWCQCG
SCLPSQLPESHRCLEELCCRKKPGACITTSELFRKLVLSRHVLQFLLLYQEPLLALDVDS
TNSRLRHCAYRCYATWRFGSQDMADFAILPSCCRWRIRKEFPKSEGQYSGFKSPY
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM254160
n/a
NameBDBM254160
Synonyms:US10112937, Example 40 | US10150765, Example 40 | US10703749, Example 11 | US9464084, 40
TypeSmall organic molecule
Emp. Form.C20H15ClF4N4O
Mol. Mass.438.806
SMILESC[C@H]1N(CCc2c1ncn2-c1ccc(F)cn1)C(=O)c1cccc(c1Cl)C(F)(F)F |r|
Structure
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