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Target
P2X purinoceptor 7
Ligand
BDBM254139
Substrate
n/a
Meas. Tech.
ChEMBL_1616307 (CHEMBL3858376)
IC50
34±n/a nM
Citation
 Swanson, DM; Savall, BM; Coe, KJ; Schoetens, F; Koudriakova, T; Skaptason, J; Wall, J; Rech, J; Deng, X; De Angelis, M; Everson, A; Lord, B; Wang, Q; Ao, H; Scott, B; Sepassi, K; Lovenberg, TW; Carruthers, NI; Bhattacharya, A; Letavic, 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 Chem 59:8535-48 (2016) [PubMed]  Article 
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:
BDBM254139
Synonyms:
US10112937, Example 17 | US10150765, Example 17 | US10703749, Example 17 | US9464084, 17
Type:
Small organic molecule
Emp. Form.:
C20H16ClF3N4O
Mol. Mass.:
420.815
SMILES:
CC1N(CCc2c1ncn2-c1ccccn1)C(=O)c1cccc(c1Cl)C(F)(F)F
Structure:
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